💥 Exam 3
Pain and the brain: analgesics, anti-inflammatories, substance use, the neurodegenerative drugs, and mental health.
Modules 4–5 · 50 questions · 39 drugs · 21 concepts
Module 4: Pain and Substance Abuse
What are the adverse effects of opioid agonists?🚨 DANGER
RESPIRATORY DEPRESSION is the one that kills; CONSTIPATION is the one that never goes away. Also sedation, hypotension and light-headedness, dizziness, nausea and vomiting, sweating, pruritus, urinary retention, miosis, plus tolerance and physical dependence.
- SEDATION ALWAYS PRECEDES RESPIRATORY DEPRESSION. Rising drowsiness is your early warning. Assess sedation level along with respiratory rate, and hold the dose for excessive sedation rather than waiting for the respiratory rate to fall.
- Tolerance develops to nearly every effect EXCEPT constipation and miosis. Start a stimulant laxative plus a stool softener at the same time as the opioid, not after the patient is impacted.
- Overdose triad: pinpoint pupils, respiratory depression, and decreased level of consciousness. Naloxone is the reversal agent.
- Boxed warning: combining an opioid with benzodiazepines, alcohol, or any other CNS depressant markedly increases the risk of profound sedation, respiratory depression, and death.
- Highest-risk patients: opioid-naive, older adults, obesity or sleep apnea, renal or hepatic impairment, and the first 24 hours after starting or increasing a dose.
- Meperidine is generally avoided: its metabolite normeperidine is neurotoxic and causes seizures, especially in older adults and renal impairment. Morphine is a Schedule II controlled substance with real diversion risk; follow waste and countersign policy exactly.
Sedation before respiration. Pinpoint pupils, pinpoint breathing. And they will be constipated forever.
What are the treatment options for acute opioid overdose?🚨 DANGER
NALOXONE (Narcan), an opioid antagonist that displaces the opioid off its receptors, PLUS airway and ventilatory support. Airway first: bag-mask ventilation and oxygen while the naloxone is drawn up. Titrate naloxone to adequate respirations, not to full wakefulness.
- Naloxone has a SHORTER DURATION OF ACTION THAN MOST OPIOIDS, so repeat doses or a continuous infusion are often needed. Never leave the patient or discharge them after one dose - re-narcotization is the classic exam answer.
- Routes: IV (fastest), IM, subcutaneous, and intranasal. Take-home intranasal naloxone should be prescribed to anyone on high-dose or long-term opioids and to their household.
- Giving too much too fast produces ACUTE WITHDRAWAL: agitation, pain, hypertension, tachycardia, vomiting, diaphoresis, and tremors. In postoperative patients the textbook warns of hypotension, hypertension, ventricular tachycardia and fibrillation, pulmonary edema, and cardiac arrest.
- In a chronic-pain or postop patient, dilute and give small increments, watching the respiratory rate. In a street overdose, the priority is simply reversing apnea.
- It works on opioids ONLY. It will not reverse benzodiazepines, alcohol, or stimulants. If the patient does not respond, look for another cause. (Flumazenil reverses benzodiazepines but is rarely used because it can precipitate seizures.)
- Naltrexone is a different drug: long-acting, oral or monthly IM, used for maintenance treatment of opioid and alcohol use disorder, NOT for acute overdose.
Airway, then Narcan, then stay: the antidote wears off before the opioid does.
What are the adverse effects of non-steroidal anti-inflammatory drugs (NSAIDs)?🚨 DANGER
GI ULCERATION AND BLEEDING is the classic (from COX-1 inhibition removing gastric protection). Also renal impairment and fluid retention, increased blood pressure, increased CARDIOVASCULAR thrombotic risk (boxed warning), bleeding from antiplatelet effect, hypersensitivity, and tinnitus with aspirin.
- GI risk is higher with: high dose, long duration, more than one NSAID at a time, age 60 and over, prior ulcer or GI bleed, concurrent anticoagulant or corticosteroid, and three or more alcoholic drinks a day. Take with food or milk and consider a PPI for high-risk patients.
- Teach the patient to report black tarry stools, coffee-ground emesis, or new abdominal pain. GI bleeding from NSAIDs is often PAINLESS until it is severe.
- RENAL: NSAIDs block the prostaglandins that keep the afferent arteriole dilated, so they cause acute kidney injury, sodium and water retention, edema, hyperkalemia, and worsening heart failure. The 'triple whammy' of an NSAID plus an ACE inhibitor or ARB plus a diuretic is a common cause of AKI.
- CARDIOVASCULAR boxed warning: all NSAIDs except aspirin increase the risk of MI and stroke, even in the first weeks. Contraindicated for pain after coronary artery bypass grafting.
- ASPIRIN specifics: irreversible platelet inhibition for the life of the platelet (7 to 10 days), tinnitus as an early sign of salicylism, and REYE SYNDROME - never give aspirin to a child or teenager with chickenpox or a flu-like illness.
- KETOROLAC is limited to 5 DAYS TOTAL by any route because of GI and renal toxicity. Celecoxib is COX-2 selective, so less GI injury, but it still carries the cardiovascular and renal risks and is avoided in sulfonamide allergy. Aspirin-exacerbated respiratory disease (the 'aspirin triad': asthma, nasal polyps, aspirin sensitivity) means all NSAIDs must be avoided.
NSAIDs: Bleeding stomach, Beat-up Kidneys, Blood pressure up, and Blood clots. Aspirin adds ringing ears and Reye's.
How does the pharmacological treatment differ for an acute migraine compared to the prophylaxis of migraines?⭐ HIGH YIELD
ACUTE (abortive) treatment is taken AT THE ONSET of a migraine to stop the attack in progress: TRIPTANS, ergot alkaloids, NSAIDs, acetaminophen, and antiemetics. PROPHYLAXIS is taken EVERY DAY whether or not there is a headache, to reduce how often attacks happen: beta blockers, topiramate, valproate, amitriptyline, and CGRP monoclonal antibodies.
- Triptan rules (textbook): give at the ONSET of the migraine, may repeat ONCE after 2 hours, not to exceed 200 mg of sumatriptan per day. Routes are oral, subcutaneous, and nasal spray. Adverse effects: dizziness, vertigo, somnolence, nausea, vomiting, chest discomfort, and angina.
- Triptans and ergots are VASOCONSTRICTORS, so both are contraindicated in coronary artery disease, uncontrolled hypertension, peripheral vascular disease, and stroke history. Ergotamine is additionally contraindicated in renal or hepatic dysfunction. NEVER give a triptan and an ergot within 24 hours of each other.
- Triptans plus SSRIs, SNRIs, or other serotonergic drugs raise SEROTONIN SYNDROME risk. Chest tightness after a triptan is usually not cardiac, but it must be evaluated the first time.
- MEDICATION OVERUSE (rebound) HEADACHE: using abortive drugs more than 2 to 3 days a week makes headaches more frequent. That frequency is itself the trigger for starting prophylaxis.
- Prophylaxis is indicated at roughly 4 or more migraine days a month, or when attacks are disabling despite abortive therapy. It takes 4 to 8 WEEKS to judge whether it is working, so tell the patient not to quit early.
- Non-drug measures matter for both: identify and avoid triggers, regular sleep and meals, hydration, stress management, and a headache diary. Newer options: gepants (ubrogepant, rimegepant) and lasmiditan for acute attacks, which do not vasoconstrict, and onabotulinumtoxinA for chronic migraine.
| ACUTE / abortive | PROPHYLAXIS / preventive |
|---|
| Taken at the first sign of an attack | Taken every day regardless of symptoms |
| Triptans: sumatriptan, rizatriptan, zolmitriptan | Beta blockers: PROPRANOLOL, metoprolol, timolol |
| Ergot alkaloids: ergotamine, dihydroergotamine | Anticonvulsants: TOPIRAMATE, valproate/divalproex |
| NSAIDs, acetaminophen, aspirin-acetaminophen-caffeine | Antidepressants: amitriptyline, venlafaxine |
| Antiemetics: metoclopramide, prochlorperazine | CGRP monoclonal antibodies: erenumab, fremanezumab, galcanezumab; atogepant |
| Gepants (ubrogepant, rimegepant), lasmiditan | Candesartan; onabotulinumtoxinA for chronic migraine |
| Goal: stop THIS headache | Goal: fewer and milder headaches over months |
Abortive = at the onset, once, maybe twice. Preventive = every day, and give it 8 weeks.
Define opioid agonist, opioid partial agonist, and opioid antagonist. Give examples of drugs in each pharmacological category.⭐ HIGH YIELD
AGONIST: binds the opioid receptor and fully activates it, producing full analgesia with no ceiling (morphine, fentanyl, hydromorphone, oxycodone, hydrocodone, codeine, methadone). PARTIAL AGONIST/agonist-antagonist: activates the receptor only partially, so there is a CEILING effect (buprenorphine, butorphanol, nalbuphine, pentazocine). ANTAGONIST: binds and blocks with no activation (naloxone, naltrexone).
- The ceiling effect is the point of partial agonists: past a certain dose, more drug gives no more analgesia AND no more respiratory depression, so the overdose risk is lower. They also have lower abuse potential.
- THE TRAP: giving a partial agonist or agonist-antagonist to someone who is physically dependent on a full agonist DISPLACES the full agonist and PRECIPITATES ACUTE WITHDRAWAL. Always ask about current opioid use before giving nalbuphine, butorphanol, or buprenorphine.
- Buprenorphine (with or without naloxone, as Suboxone) is a mainstay of opioid use disorder treatment; methadone is the full-agonist alternative and requires a certified program plus QT monitoring.
- Naloxone is short-acting and used for ACUTE overdose. Naltrexone is long-acting (daily oral or monthly IM) and used for MAINTENANCE in opioid and alcohol use disorder. Naltrexone requires 7 to 10 opioid-free days first or it will precipitate withdrawal.
- Peripherally acting antagonists (methylnaltrexone, naloxegol, alvimopan) treat opioid-induced constipation without reversing analgesia, because they do not cross the blood-brain barrier.
- Receptor shorthand: mu receptors give analgesia, euphoria, respiratory depression, constipation, and dependence. Kappa gives analgesia and sedation with less euphoria, which is why kappa agonist / mu antagonist drugs like nalbuphine and butorphanol behave the way they do.
| Category | What it does at the receptor | Examples |
|---|
| Full agonist | Fully activates mu; no analgesic ceiling | morphine, hydromorphone, fentanyl, oxycodone, hydrocodone, codeine, methadone, meperidine, tramadol (weak) |
| Partial agonist / agonist-antagonist | Partial mu activation or kappa agonist + mu antagonist; CEILING effect; can precipitate withdrawal | buprenorphine, butorphanol, nalbuphine, pentazocine |
| Antagonist | Binds and blocks, no activation; reverses effects | naloxone (acute overdose), naltrexone (maintenance), methylnaltrexone (constipation only) |
Full agonist = no ceiling. Partial = ceiling, and it will yank a dependent patient into withdrawal. Antagonist = pure block.
💉 AcetaminophenBLACK BOX
Nonopioid analgesic, antipyretic, Nonsalicylate, paraaminophenol derivative
What it is for
Mild to moderate pain or fever, arthralgia, dental pain, dysmenorrhea, headache, myalgia, osteoarthritis Unlabeled: Migraine
How it works
Activates descending serotonergic inhibitory pathway in CNS; antipyretic action results from (hypothalamic heat-regulating center)
Watch for
CNS: Agitation (child) (IV); headache, fatigue, anxiety (IV) RESP: Dyspnea (IV), atelectasis (child) (IV) CV: Hyper- and hypotension (IV) GI: Nausea, vomiting, abdominal pain …
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 AmitriptylineBLACK BOX
Antidepressant—tricyclic, Tertiary amine
What it is for
Major depressive disorder
How it works
Blocks reuptake of norepinephrine, serotonin into nerve endings, thereby increasing action of norepinephrine, serotonin in nerve cells
Watch for
CNS: Dizziness, drowsiness, confusion, headache, anxiety, tremors, weakness, insomnia, EPS (geriatric patients), seizures, suicidal thoughts, anxiety CV: Orthostatic hypotension, ECG changes, tachycardia, hypertension, palpitations, dysrhythmias, QT prolongation EENT: Blurred vision, tinnitus …
Teaching
- To take medication as directed (usually at bedtime); not to double dose; that therapeutic effects may take 2-3 wk; not to discontinue medication quickly after long-term u …
- To use caution when driving, performing other activities that require alertness because of drowsiness, dizziness, blurred vision; to avoid rising quickly from sitting to …
- To avoid alcohol, other CNS depressants
- To wear sunscreen or large hat when outdoors; photosensitivity occurs
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 AspirinHIGH ALERTBLACK BOX
Opiate analgesic, Semisynthetic derivative
What it is for
Moderate to severe pain Unlabeled: Postherpetic neuralgic (cont rel)
How it works
Inhibits ascending pain pathways in CNS, increases pain threshold, alters pain perception
Watch for
CNS: Drowsiness, dizziness, confusion, headache, sedation, euphoria, fatigue, abnormal dreams/thoughts, hallucinations CV: Palpitations, bradycardia, change in B/P EENT: Tinnitus, blurred vision, miosis, diplopia GI: Nausea, vomiting, anorexia, constipation, cramps, gastritis, dyspepsia …
Teaching
- To report any symptoms of CNS changes, allergic reactions
- That physical dependency may result from extended use
- That withdrawal symptoms may occur after long-term use: nausea, vomiting, cramps, fever, faintness, anorexia
- To avoid CNS depressants, alcohol
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 BaclofenBLACK BOX
Skeletal muscle relaxant, central acting, GABA chlorophenyl derivative
What it is for
Spasticity with spinal cord injury, multiple sclerosis Unlabeled: Neuropathic pain, trigeminal neuralgia
How it works
Inhibits synaptic responses in CNS by stimulating GABAb receptor subtype, which decreases neurotransmitter function; decreases frequency, severity of muscle spasms
Watch for
CNS: Dizziness, weakness, fatigue, drowsiness, headache, disorientation, insomnia, paresthesias, tremors; seizures (IT) CV: Hypotension, bradycardia, flushing, edema EENT: Nasal congestion, blurred vision, tinnitus GI: Nausea, constipation, dry mouth, anorexia, weight gain GU: Urinary frequency …
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 Benztropine
Anticholinergic, antiparkinson agent, Tertiary amine
What it is for
Parkinson’s symptoms, EPS associated with neuroleptic products, acute dystonic reactions
How it works
Blockade of central acetylcholine receptors, balances cholinergic activity
Watch for
CNS: Hallucinations, depression, dizziness, memory loss; confusion; delirium (geriatric headache, sedation) CV: Palpitations, tachycardia, hypotension, bradycardia EENT: Blurred vision, photophobia GI: Dry mouth, constipation …
Teaching
- To report urinary hesitancy/retention, dysuria
- That tablets may be crushed, mixed with food; may take whole dose at bedtime if approved by prescriber
- Not to discontinue product abruptly; to taper off over 1 wk or withdrawal symptoms may occur (EPS, tremors, insomnia, tachycardia, restlessness); to take as directed; not …
- To avoid driving, other hazardous activities; drowsiness/dizziness may occur
🔗 Full card in the drug guide
💉 BuprenorphineHIGH ALERTBLACK BOX
Opioid analgesic, partial agonist, Thebaine derivative
What it is for
Moderate to severe pain, opiate agonist withdrawal/dependence
How it works
Depresses pain impulse transmission at the spinal cord level by interacting with opioid receptors, partial agonist at μ-opioid receptor
Watch for
CNS: Drowsiness, dizziness, confusion, headache, sedation, euphoria, hallucinations, strange dreams CV: Palpitations, QT prolongation, hypo/hypertension EENT: Tinnitus, blurred vision, miosis, diplopia GI: Nausea, vomiting, anorexia, constipation, dry mouth …
Teaching
- To report any symptoms of CNS changes, allergic reactions
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 BupropionBLACK BOX
Antidepressant—miscellaneous smoking deterrent, Aminoketone
What it is for
Depression (Wellbutrin), smoking cessation (Zyban); seasonal affective disorder, substance abuse, glaucoma, smoking, cardiac disease, heart failure Unlabeled: ADHD (adult)
How it works
Inhibits reuptake of DOPamine, norepinephrine, serotonin
Watch for
CNS: Headache, agitation, dizziness, akinesia, confusion, seizures, delusions, insomnia, sedation, tremors, suicidal/homicidal ideation, flushing CV: Dysrhythmias, hypertension, palpitations, tachycardia, hypotension, chest pain, chills EENT: Blurred vision, auditory disturbance GI: Nausea …
Teaching
- That therapeutic effects may take 2-4 wk; not to increase dose without prescriber’s approval; that treatment for smoking cessation lasts 7-12 wk
- To use caution when driving, performing other activities that require alertness; sedation, blurred vision may occur
- To avoid alcohol, other CNS depressants; alcohol may increase risk of seizures
- Not to chew, crush tablets
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 CelecoxibHIGH ALERTBLACK BOX
Nonsteroidal antiinflammatory, antirheumatic, COX-2 inhibitor
What it is for
Acute, chronic rheumatoid arthritis, osteoarthritis, acute pain, primary dysmenorrhea, ankylosing spondylitis, juvenile rheumatoid arthritis (JRA); acute migraine (Elyxyb)
How it works
Inhibits prostaglandin synthesis by selectively inhibiting cyclooxygenase-2 (COX-2), an enzyme needed for biosynthesis
Watch for
CNS: Fatigue, nervousness, insomnia, headache CV: Stroke, MI, HF, hypertension, fluid retention GI: Nausea, anorexia, dry mouth, GI bleeding/ulceration INTEG: Serious (sometimes fatal) Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis, rash
🔗 Full card in the drug guide
💉 DantroleneHIGH ALERTBLACK BOX
Skeletal muscle relaxant, direct acting, Hydantoin
What it is for
Spasticity in multiple sclerosis, stroke, spinal cord injury, cerebral palsy, malignant hyperthermia Black Box Warning: Hepatotoxicity
🔗 Full card in the drug guide
Disulfiram🚨 DANGER
Disulfiram (Antabuse) is an aversion therapy for ALCOHOL USE DISORDER. It blocks aldehyde dehydrogenase, so acetaldehyde accumulates and drinking causes a violently unpleasant reaction. It does not reduce craving; it works purely by deterrence.
- THE DISULFIRAM REACTION starts within 10 to 30 minutes of any alcohol: intense flushing, throbbing headache, nausea and copious vomiting, sweating, palpitations, tachycardia, dyspnea, chest pain, blurred vision, weakness, confusion, and hypotension. Severe reactions cause respiratory depression, arrhythmias, seizures, MI, and death.
- TEACH EVERY HIDDEN SOURCE OF ALCOHOL: mouthwash, cough and cold syrups, elixirs, vanilla and other flavoring extracts, sauces, vinegars, aftershave, colognes, hand sanitizer, and some topical preparations. Even skin exposure can trigger it.
- The effect persists for up to 14 DAYS after the last dose, so the alcohol ban continues for two weeks after stopping.
- The patient must be ABSTINENT for at least 12 hours (and free of alcohol on the breath) before the first dose, and must consent knowingly. Never give it to someone who is intoxicated or who does not know they are getting it.
- Also causes a metallic or garlic aftertaste, drowsiness, headache, and rarely hepatotoxicity and peripheral neuropathy. Monitor LFTs at baseline and periodically. Contraindicated in severe cardiac disease and psychosis.
- Interactions: raises phenytoin, warfarin, and isoniazid levels. Metronidazole and some cephalosporins cause a disulfiram-LIKE reaction with alcohol on their own; so do sulfonylureas. Other options for alcohol use disorder work differently: naltrexone reduces craving and reward, and acamprosate helps maintain abstinence.
Disulfiram doesn't stop the craving, it punishes the drink. And 'alcohol' includes the mouthwash.
💉 Donepezil
Anti-Alzheimer’s agent, Reversible cholinesterase inhibitor
What it is for
Mild to severe dementia with Alzheimer’s disease
How it works
Elevates acetylcholine concentrations (cerebral cortex) by slowing degradation of acetylcholine released in cholinergic neurons; does not alter underlying dementia
Watch for
CNS: Dizziness, insomnia, headache, fatigue, abnormal dreams, syncope, seizures, drowsiness, agitation, depression, confusion, hallucinations CV: Atrial fibrillation, hypo/hypertension GI: Nausea, vomiting, anorexia, diarrhea, abdominal pain, weight gain GU: Urinary frequency INTEG: Rash, flushing …
Teaching
- To report side effects: twitching, nausea, vomiting, sweating, dizziness; indicates cholinergic crisis or overdose
- That continuing follow-up will be needed
- To use product exactly as prescribed, not to use with other products unless approved by prescriber
- To notify prescriber of nausea, vomiting, diarrhea (dose increase or beginning treatment), or rash
🔗 Full card in the drug guide
💉 Entacapone
Antiparkinson agent, COMT inhibitor
What it is for
Parkinson’s disease for those experiencing end-of-dose, decreased effect as adjunct to levodopa/carbidopa
🔗 Full card in the drug guide
💉 IbuprofenBLACK BOX
NSAID, Propionic acid derivative
What it is for
Inflammatory disorders: Rheumatoid arthritis, osteoarthritis, primary dysmenorrhea, dental pain, musculoskeletal disorders, fever, migraine, patent ductus arteriosus, headache Unlabeled: Ankylosing spondylitis, bone pain, cystic fibrosis, gouty arthritis …
How it works
Inhibits COX-1, COX-2 by blocking arachidonate; analgesic, antiinflammatory, antipyretic
Watch for
CNS: Headache, dizziness, drowsiness, fatigue CV: Tachycardia, peripheral edema, palpitations, dysrhythmias, CV thrombotic events, MI, stroke, HF EENT: Tinnitus, hearing loss, blurred vision GI: Nausea, anorexia, vomiting, diarrhea, jaundice, constipation, flatulence, cramps, dry mouth …
Teaching
- To use sunscreen, sunglasses, and protective clothing to prevent photosensitivity, photophobia
- To report blurred vision, ringing, roaring in ears (may indicate toxicity); that eye and hearing tests should be done during long-term therapy
- To avoid driving, other hazardous activities if dizziness or drowsiness occurs
🔗 Full card in the drug guide
Levodopa/carbidopa⭐ HIGH YIELD
Levodopa is a dopamine precursor that crosses the blood-brain barrier and is converted to dopamine to treat Parkinson's disease. Carbidopa blocks that conversion in the PERIPHERY, so more levodopa reaches the brain and there is far less nausea.
- Avoid HIGH-PROTEIN meals with the dose: dietary amino acids compete with levodopa for absorption and blunt the effect.
- Harmless but alarming: sweat, saliva, and urine may turn dark red, brown, or black. Warn the patient in advance.
- Orthostatic hypotension is common. Rise slowly and use fall precautions.
- Long-term: dyskinesias, wearing-off, and the on-off phenomenon (abrupt loss of effect). Doses must be given ON TIME, to the minute.
- Do NOT stop abruptly: risk of a neuroleptic malignant-like syndrome. Avoid with MAOIs (hypertensive crisis) and with antipsychotics or metoclopramide, which are dopamine blockers that cancel it out. Report hallucinations, confusion, sudden sleep attacks, and impulse-control behaviors such as gambling, spending, and hypersexuality.
Carbidopa is the bodyguard: it keeps levodopa from being mugged before it reaches the brain.
💉 Memantine
Anti-Alzheimer’s agent, N-methyl-D-aspartate receptor antagonist
What it is for
Moderate to severe dementia in Alzheimer’s disease
How it works
Antagonist action of CNS NMDA receptors that may contribute to the symptoms of Alzheimer’s disease
Watch for
CNS: Dizziness, confusion, headache, stroke CV: Hypertension, HF GI: Vomiting, constipation INTEG: Rash MISC: Back pain, fatigue, flulike symptoms
Teaching
- To report side effects: restlessness, psychosis, visual hallucinations, stupor, LOC; may indicate overdose
- To use product exactly as prescribed; to avoid alcohol, nicotine
- To use oral sol dispenser provided
- To avoid OTC, herbal products unless approved by prescriber
🔗 Full card in the drug guide
💉 MorphineHIGH ALERTBLACK BOX
Opioid analgesic, Alkaloid
What it is for
Moderate to severe pain Unlabeled: Agitation, bone/dental pain, dyspnea in end-stage cancer or pulmonary disease, sedation induction, rapid-sequence intubation
How it works
Depresses pain impulse transmission at the spinal cord level by interacting with opioid receptors
Watch for
CNS: Drowsiness, dizziness, confusion, headache, sedation, euphoria, insomnia, seizures CV: Palpitations, bradycardia, change in B/P, shock, cardiac arrest, chest pain, hypo/hypertension, edema, tachycardia EENT: Blurred vision, miosis, diplopia ENDO: Gynecomastia GI: Nausea, vomiting, anorexia …
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 Naloxone
Opioid antagonist, antidote, Thebaine derivative
What it is for
Respiratory depression induced by opioids, opiate agonist overdose Unlabeled: Pruritus (opiate induced)
How it works
Competes with opioids at opiate receptor sites
Watch for
CV: Rapid pulse, ventricular tachycardia, fibrillation, hypo/hypertension GI: Nausea, vomiting CNS: Headache, seizures MS: Pain INTEG: Injection site reactions MISC: Withdrawal symptoms in those dependent EENT: Nasal dryness
Teaching
- When patient is lucid, about the reasons for, expected results of product; for nasal administration, teach family, caregivers correct use, use of autoinjector
- Opioid emergency:
- Teach patient and family increased sleepiness, coma, trouble breathing are a sign of overdose; discuss family’s use of this product for overdose
🔗 Full card in the drug guide
💉 Pramipexole
Antiparkinson agent, DOPamine-receptor agonist, non-ergot
What it is for
Idiopathic Parkinson’s disease, restless legs syndrome
How it works
Selective agonist for D2 receptors (presynaptic/postsynaptic sites); binding at D3 receptor contributes to antiparkinson effects
Watch for
CNS: Agitation, insomnia, psychosis, hallucinations, depression, dizziness, headache, confusion, amnesia, dream disorder, asthenia, dyskinesia, hypersomnolence, sudden sleep onset, impulse control disorders CV: Orthostatic hypotension, edema, syncope, tachycardia, increased B/P, heart rate …
Teaching
- That therapeutic effects may take several weeks to a few months
- To change positions slowly to prevent orthostatic hypotension
- To use product exactly as prescribed; if product is discontinued abruptly, parkinsonian crisis may occur; to avoid alcohol, OTC sleeping products
- To notify prescriber if pregnancy is planned or suspected
🔗 Full card in the drug guide
💉 Pregabalin
Anticonvulsant, γ-Aminobutyric acid (GABA) analog
What it is for
Neuropathic pain associated with spinal cord injury/diabetic peripheral neuropathy, partial-onset seizures, postherpetic neuralgia, fibromyalgia
How it works
Binds to high-voltage–gated calcium channels in CNS tissues; this may lead to anticonvulsant action similar to the inhibitory neurotransmitter GABA; anxiolytic, analgesic, and antiepileptic properties
Watch for
CNS: Dizziness, drowsiness abnormal thinking, suicidal ideation EENT: Dry mouth, blurred vision, sinusitis GI: Constipation, abdominal pain, weight gain, nausea, vomiting, increased appetite GU: Gynecomastia HEMA: Thrombocytopenia MS: Back pain, rhabdomyolysis, myopathy OTHER: Pruritus …
Teaching
- To carry emergency ID stating patient’s name, products taken, condition, prescriber’s name and phone number
- To avoid driving, other activities that require alertness because dizziness, drowsiness may occur, to obtain clearance from provider if driving is acceptable
- Not to discontinue medication quickly after long-term use; to taper over ≥1 wk; that withdrawal-precipitated seizures may occur; not to double doses if dose is missed, to …
- To notify prescriber if pregnancy is planned or suspected; to avoid breastfeeding
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 SelegilineBLACK BOX
Antiparkinson agent, antidepressant, MAOI, type B
What it is for
Adjunct management of Parkinson’s disease for patients being treated with levodopa/carbidopa who had poor response to therapy; depression (transdermal)
How it works
Increased dopaminergic activity by inhibition of MAO type B activity; not fully understood
Watch for
CNS: Increased tremors, tardive dyskinesia, dystonic symptoms, hallucinations, dizziness, mood changes, nightmares, delusions, serotonin syndrome, headache, migraine, confusion, anxiety, suicide in child/adolescent, suicidal ideation in adults CV: Orthostatic hypotension, angina pectoris …
Teaching
- To change positions slowly to prevent orthostatic hypotension
- Hypertensive crisis: to notify prescriber immediately of nausea, vomiting, sweating, agitation, change in mental status, headache, chest pain
- Serotonin syndrome: to report twitching, sweating, shivering, diarrhea to prescriber immediately
- To use product exactly as prescribed; that if discontinued abruptly, parkinsonian crisis may occur
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 Sumatriptan
Antimigraine agent, 5-HT1B/D receptor agonist, abortive agent, triptan
What it is for
Acute treatment of migraine with/without aura and cluster headache
How it works
Binds selectively to the vascular 5-HT1B/D receptor subtype; exerts antimigraine effect; causes vasoconstriction in cranial arteries
Watch for
CNS: Tingling, hot sensation, burning, feeling of pressure, tightness, numbness, dizziness, sedation, headache, anxiety, fatigue, cold sensation CV: Flushing, MI, hypo-/hypertension EENT: Throat, mouth, nasal discomfort …
Teaching
- To report chest pain, tightness; sudden, severe abdominal pain; swelling of eyelids, face, lips; skin rash to prescriber immediately
- To notify prescriber if pregnancy is planned or suspected; to use contraception while taking product
- Risk of medication overuse: do not use for abortive headache treatments more than 10 days/mo (ergotamines, triptans, opioids, or combinations)
- Nasal spray: to use 1 spray in 1 nostril; may repeat if headache returns; not to repeat if pain continues after 1st dose
🔗 Full card in the drug guide
💉 TramadolHIGH ALERTBLACK BOX
Analgesic—miscellaneous
What it is for
Management of moderate to severe pain, chronic pain Unlabeled: Restless legs syndrome (RLS), premature ejaculation
How it works
Binds to μ-opioid receptors, inhibits reuptake of norepinephrine, serotonin
Watch for
CNS: Dizziness, CNS stimulation, somnolence, headache, anxiety, confusion, euphoria, seizures, hallucinations, sedation, neuroleptic malignant syndrome–like reactions CV: Vasodilation, orthostatic hypotension, tachycardia, hypertension, abnormal ECG EENT: Visual disturbances GI: Nausea …
Teaching
- Before taking, inform health care provider of any history of head injury; seizures; liver, kidney, thyroid problems; problems in urinating; pancreas or gallbladder proble …
- Not to take other prescription medications, OTC products, vitamins, or herbal supplements without approval from health care provider
- To take exactly as prescribed by health care provider; not to take more than prescribed dose and not to take >8 tablets/day. If dose is missed, to take the next dose at u …
- To notify health care provider if the prescribed does not control pain
🔗 Full card in the drug guide
💉 Varenicline
Smoking cessation agent, Nicotine receptor agonist
What it is for
Adjunct to psychosocial interventions for tobacco cessation (smoking); dry eye disease (Tyrvaya)
How it works
Partial agonist for nicotine receptors; partially activates receptors to help curb cravings; occupies receptors to prevent nicotine binding
Watch for
CNS: Headache, agitation, dizziness, insomnia, abnormal dreams, fatigue, malaise, behavioral changes, depression, homicidal ideation, suicidal ideation, amnesia, hallucinations, hostility, mania, psychosis, tremors, seizures, stroke CV: Dysrhythmias, MI EENT: Blurred vision GI: Nausea, vomiting …
Teaching
- To set a date to quit smoking and to initiate treatment 1 wk before that date
- That treatment for smoking cessation lasts 12 wk and that another 12 wk may be required
- To use caution when driving, performing other activities requiring alertness; blurred vision may occur
- How to titrate product
🔗 Full card in the drug guide
Module 5: Mental Health Drugs
What are the pharmacological treatment options for anxiety disorders?⭐ HIGH YIELD
SSRIs and SNRIs are FIRST-LINE for long-term treatment of anxiety disorders. BENZODIAZEPINES are for short-term or breakthrough use only. Other options: buspirone, hydroxyzine, propranolol for performance anxiety, and gabapentin or pregabalin as adjuncts. Cognitive behavioral therapy is at least as effective as medication.
- SSRIs and SNRIs take 4 to 6 WEEKS to work and can transiently WORSEN anxiety in the first 1 to 2 weeks. Start low, go slow, and warn the patient so they do not quit on day 3.
- Benzodiazepines (lorazepam, alprazolam, clonazepam, diazepam) work in minutes, which makes them useful for acute panic, but they are Schedule IV, cause tolerance and physical dependence, and should be prescribed for SHORT PERIODS ONLY, typically 2 to 4 weeks per the textbook. Never stop them abruptly: withdrawal can cause seizures.
- Benzodiazepine teaching: no alcohol or other CNS depressants, no driving for 24 to 48 hours after a dose, and do not get out of bed unassisted within 8 hours of a dose because of fall risk. Older adults and children may have PARADOXICAL reactions (agitation, tremor, hallucinations). Antidote is flumazenil.
- BUSPIRONE is the non-sedating, non-addictive alternative: no dependence, no CNS depression, no PRN use. It must be taken scheduled and takes 2 to 4 weeks to work. Avoid grapefruit juice.
- All antidepressants carry a BOXED WARNING for increased suicidality in children, adolescents, and young adults. Monitor closely at initiation and with every dose change, and teach family to report sudden changes in mood or behavior.
- Avoid St John's wort with SSRIs or SNRIs (serotonin syndrome). Avoid caffeine, alcohol, and stimulants, which worsen anxiety.
| Option | Onset | Role |
|---|
| SSRIs: sertraline, escitalopram, paroxetine, fluoxetine | 4 to 6 weeks | FIRST-LINE maintenance for GAD, panic, social anxiety, OCD, PTSD |
| SNRIs: venlafaxine, duloxetine | 4 to 6 weeks | First-line alternative; duloxetine also treats neuropathic pain |
| Benzodiazepines: lorazepam, alprazolam, clonazepam | Minutes | Short-term/bridge only; dependence, falls, no abrupt stop |
| Buspirone | 2 to 4 weeks | Scheduled dosing, no dependence, no sedation; not for PRN or panic |
| Hydroxyzine | Within an hour | PRN, non-addictive; sedating and anticholinergic |
| Propranolol | About an hour | Blocks the physical symptoms (tremor, palpitations) of performance anxiety |
SSRIs for the long game, benzos for the bridge, buspirone if you can't use either. Not PRN.
What are the risk factors for developing serotonin syndrome?🚨 DANGER
The main risk factor is COMBINING SEROTONERGIC DRUGS, or starting or increasing the dose of one. The highest-risk combinations are an SSRI or SNRI with an MAOI, with a triptan, with tramadol, with linezolid, or with St John's wort.
- The textbook names the setup precisely: concurrent use of serotonergic drugs, drugs that impair serotonin metabolism (including MAOIs), or antipsychotics and other dopamine antagonists, with SSRIs and SNRIs.
- MAOI plus any other serotonergic drug is the single most dangerous combination and requires a WASHOUT: 14 days between an MAOI and most SSRIs, and 5 WEEKS after fluoxetine because of its long half-life.
- Other risk factors: overdose or intentional ingestion, dose escalation, adding a CYP450 inhibitor that raises the level of a serotonergic drug, and older age or hepatic impairment.
- The full serotonergic drug list: SSRIs, SNRIs, TCAs, MAOIs, trazodone, buspirone, triptans, TRAMADOL, meperidine, fentanyl, dextromethorphan, ondansetron and metoclopramide, lithium, LINEZOLID (an antibiotic that is a weak MAOI), methylene blue, St John's wort, ginseng, MDMA and cocaine.
- Onset is FAST: usually within 6 to 24 hours of the new drug or dose change. That timing is what distinguishes it from neuroleptic malignant syndrome, which develops over days to weeks.
- Prevention: reconcile every medication including OTC cough syrup and herbal supplements, honor washout periods, and teach the patient to tell every prescriber about their antidepressant.
Two serotonin drugs is the setup. MAOI plus anything is the disaster. Wash out 14 days, 5 weeks for fluoxetine.
What signs and symptoms are associated with serotonin syndrome?🚨 DANGER
Three categories, and they come on FAST (within 6 to 24 hours): MENTAL STATUS CHANGES (agitation, confusion, hallucinations, anxiety), AUTONOMIC INSTABILITY (hyperthermia, tachycardia, labile blood pressure, diaphoresis, dilated pupils, diarrhea), and NEUROMUSCULAR HYPERACTIVITY (hyperreflexia, CLONUS, tremor, rigidity, incoordination).
- CLONUS and HYPERREFLEXIA, worst in the lower extremities, are the findings that clinch the diagnosis. Check ankle clonus.
- GI symptoms are part of it and are easy to miss: nausea, vomiting, and diarrhea.
- Treatment: STOP all serotonergic agents immediately, supportive care, IV fluids, BENZODIAZEPINES for agitation and rigidity, active cooling for hyperthermia, and CYPROHEPTADINE as the serotonin antagonist antidote. Severe cases need intubation and paralysis.
- Do NOT give antipyretics for the fever. The hyperthermia comes from muscle activity, not from a raised hypothalamic set point.
- Most cases resolve within 24 hours once the drug is stopped. Severe cases progress to hyperthermia over 41 C, rhabdomyolysis, DIC, seizures, and death.
- Distinguish from neuroleptic malignant syndrome: serotonin syndrome comes on in HOURS with HYPERreflexia, clonus, dilated pupils, and diarrhea. NMS comes on over DAYS with LEAD-PIPE rigidity, HYPOreflexia, and normal pupils.
| Serotonin syndrome | Neuroleptic malignant syndrome |
|---|
| Onset in HOURS (6 to 24) of a new or increased serotonergic drug | Onset over DAYS to weeks after an antipsychotic |
| HYPERreflexia, CLONUS, tremor | LEAD-PIPE rigidity, bradyreflexia |
| Dilated pupils, hyperactive bowel sounds, diarrhea | Normal pupils, normal or decreased bowel sounds |
| Agitation, hypervigilance | Stupor, mutism, altered consciousness |
| Treat: stop drug, benzodiazepines, CYPROHEPTADINE, cooling | Treat: stop drug, DANTROLENE, BROMOCRIPTINE, cooling |
| Resolves in about 24 hours | Takes days to weeks to resolve |
SHIVERS: Shivering, Hyperreflexia, Increased temp, Vital sign instability, Encephalopathy, Restlessness, Sweating.
What are the risk factors for developing serotonin withdrawal (serotonin discontinuation⭐ HIGH YIELD
Antidepressant discontinuation syndrome is caused by STOPPING AN SSRI OR SNRI ABRUPTLY. The strongest risk factors are a SHORT HALF-LIFE (paroxetine and venlafaxine are the worst offenders), treatment for 4 to 6 weeks or longer, a higher dose, and previous episodes of discontinuation symptoms.
- The textbook is explicit: taper the dose when discontinuing, do not stop abruptly. That instruction appears in the boxed-warning row for the SSRIs, SNRIs, and TCAs.
- Half-life is the key variable. Paroxetine and venlafaxine have very short half-lives and cause severe symptoms. FLUOXETINE has a long half-life and an active metabolite, so it self-tapers and rarely causes it.
- Other risk factors: missed doses and poor adherence, a rapid taper, an abrupt switch between agents, and running out of a prescription. Hospital admission with medications held is a common real-world trigger.
- Prevention: taper over weeks to months depending on the drug and duration, using the smallest available dose decrements. Teach the patient never to stop on their own even if they feel better.
- It is NOT relapse and it is NOT addiction. Symptoms start 1 to 4 days after stopping and resolve within 24 hours of restarting the drug, which is how it is distinguished from returning depression (which comes back over weeks).
- The same discontinuation risk applies to benzodiazepines, beta blockers, clonidine, corticosteroids, and opioids. None of them should be stopped abruptly.
Short half-life plus a hard stop equals brain zaps. Paroxetine and venlafaxine are the worst; fluoxetine tapers itself.
What signs and symptoms are associated with serotonin withdrawal?⭐ HIGH YIELD
FINISH: Flu-like symptoms, Insomnia, Nausea, Imbalance (dizziness, vertigo), Sensory disturbances (the classic 'BRAIN ZAPS,' electric-shock sensations, paresthesias), and Hyperarousal (anxiety, agitation, irritability). Onset 1 to 4 days after stopping; duration 1 to 2 weeks.
- The textbook lists the abrupt-discontinuation effects as ANXIETY, INSOMNIA, and increased nervousness.
- Brain zaps are the pathognomonic symptom: brief electric-shock sensations in the head, often triggered by eye movement. Patients rarely volunteer this unless asked.
- Also seen: headache, sweating, tremor, vivid dreams and nightmares, crying spells, confusion, and a low mood that mimics relapse.
- It is unpleasant but not dangerous. The exception is stopping an MAOI, which can cause delirium and severe agitation.
- MANAGEMENT: restart the antidepressant (symptoms resolve within 24 hours, which confirms the diagnosis), then taper slowly. Or switch to fluoxetine and taper from there because of its long half-life.
- Distinguishing it from RELAPSE matters clinically: discontinuation symptoms start within days, include physical and sensory symptoms, and reverse immediately with the drug. Relapse takes weeks, is mostly mood symptoms, and takes weeks to reverse.
FINISH: Flu-like, Insomnia, Nausea, Imbalance, Sensory zaps, Hyperarousal. Days after stopping, gone in a day if you restart.
What clinical features are associated with extrapyramidal symptoms?⭐ HIGH YIELD
Four movement syndromes from DOPAMINE (D2) BLOCKADE: ACUTE DYSTONIA (sustained painful muscle spasms, torticollis, oculogyric crisis, laryngospasm), AKATHISIA (motor restlessness, inability to sit still), PSEUDOPARKINSONISM (tremor, rigidity, bradykinesia, shuffling gait, masklike face), and TARDIVE DYSKINESIA (involuntary lip smacking, tongue thrusting, chewing, and wavelike limb movements).
- They appear in a rough time order: dystonia in hours to days, akathisia in days to weeks, pseudoparkinsonism in weeks to a month, tardive dyskinesia after months to years.
- The textbook defines tardive dyskinesia as involuntary contraction of the oral and facial muscles (such as tongue thrusting) with wavelike movements of the extremities, and notes that EPS is often treated with anticholinergics such as BENZTROPINE and TRIHEXYPHENIDYL.
- ACUTE DYSTONIA IS THE EMERGENCY: laryngeal or pharyngeal spasm can obstruct the airway. Treat with IM or IV benztropine or diphenhydramine immediately.
- TARDIVE DYSKINESIA IS OFTEN IRREVERSIBLE and is made WORSE by anticholinergics. Screen with the AIMS (Abnormal Involuntary Movement Scale) at baseline and regularly. Treat by stopping or switching the drug; valbenazine and deutetrabenazine are approved.
- Causes: first-generation antipsychotics above all (haloperidol, fluphenazine, chlorpromazine), second-generation agents to a lesser degree (risperidone at higher doses is the worst of them), and the non-psychiatric dopamine blockers METOCLOPRAMIDE, prochlorperazine, and promethazine.
- Akathisia is frequently mistaken for worsening psychosis or anxiety and then treated with MORE antipsychotic, which makes it worse. Treat with propranolol, a benzodiazepine, or a dose reduction.
| Type | Onset | Signs | Treatment |
|---|
| Acute dystonia | Hours to about 5 days | Sustained spasm: torticollis, jaw and tongue spasm, oculogyric crisis, laryngospasm | IM/IV benztropine or diphenhydramine. AIRWAY EMERGENCY |
| Akathisia | Days to weeks | Inner restlessness, pacing, rocking, cannot sit still | Propranolol, benzodiazepine, or lower the dose |
| Pseudoparkinsonism | Weeks to about 1 month | Resting tremor, cogwheel rigidity, bradykinesia, shuffling gait, masklike face, drooling | Benztropine, trihexyphenidyl, or amantadine; lower the dose |
| Tardive dyskinesia | Months to years | Lip smacking, tongue thrusting, chewing, grimacing, wavelike limb movements | Often IRREVERSIBLE. Stop/switch drug; valbenazine, deutetrabenazine. Anticholinergics make it WORSE |
Dystonia = stuck. Akathisia = can't sit. Parkinsonism = slow. Tardive = tongue. In that order over time.
What signs and symptoms are associated with neuroleptic malignant syndrome?🚨 DANGER
NMS is a life-threatening reaction to dopamine-blocking drugs. FEVER: high FEVER (often over 40 C), Encephalopathy (altered mental status, stupor, mutism), Vital sign instability (labile BP, tachycardia, tachypnea, diaphoresis), Elevated CPK with myoglobinuria, and lead-pipe RIGIDITY.
- The textbook defines it as a potentially life-threatening adverse effect that includes high fever, unstable blood pressure, and myoglobinemia.
- Onset is over DAYS TO WEEKS, usually within the first 2 weeks of starting or increasing an antipsychotic. Contrast with serotonin syndrome, which develops in hours.
- The rigidity is 'LEAD PIPE': uniform resistance through the whole range of motion, unlike the ratcheting cogwheel rigidity of pseudoparkinsonism.
- Labs: CPK is markedly elevated (often thousands) from muscle breakdown, WBC is elevated, and myoglobinuria threatens ACUTE KIDNEY INJURY. Watch for dark cola-colored urine.
- TREATMENT: STOP the antipsychotic immediately, aggressive cooling, IV fluids to protect the kidneys, and DANTROLENE (a muscle relaxant that stops calcium release) plus BROMOCRIPTINE or amantadine (dopamine agonists) to restore dopamine tone. ICU-level supportive care.
- Causes: first-generation antipsychotics most of all (haloperidol, fluphenazine), but also second-generation agents, metoclopramide, promethazine, prochlorperazine, and ABRUPT WITHDRAWAL of levodopa or another dopamine agonist. The textbook also warns that lithium plus an antipsychotic raises neurotoxicity risk. Mortality is roughly 10 to 20% if unrecognized. Any patient on an antipsychotic with a new fever and rigidity gets NMS ruled out.
FEVER: Fever, Encephalopathy, Vitals unstable, Elevated CPK, Rigidity (lead pipe). Stop the drug, cool them, dantrolene.
How to the expected adverse effects differ between first generation and second-generation⭐ HIGH YIELD
FIRST-GENERATION (typical) antipsychotics cause MOVEMENT problems: extrapyramidal symptoms, tardive dyskinesia, and NMS, plus anticholinergic and orthostatic effects. SECOND-GENERATION (atypical) antipsychotics cause METABOLIC problems: weight gain, hyperglycemia, and hyperlipidemia, with much less EPS.
- The textbook's framing: first-generation drugs block dopamine broadly, producing tranquilizing effect plus adverse effects from blocking alpha-adrenergic, dopamine, endocrine, histamine, and muscarinic receptors. Second-generation drugs block specific D2 AND serotonin-2 receptors, causing fewer adverse effects.
- BOTH generations carry the SAME BOXED WARNING: increased risk of death in ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS, from cardiovascular events and infection. Monitor those patients closely for cardiac events and pneumonia.
- BOTH generations can cause AGRANULOCYTOSIS (the textbook states this for both), NMS, and hypersensitivity reactions, and both cause falls from sedation, motor instability, and postural hypotension.
- Metabolic monitoring for second-generation drugs: weight and BMI, waist circumference, fasting glucose and A1C, and a lipid panel at baseline and periodically. Olanzapine and clozapine are the worst; ziprasidone, aripiprazole, and lurasidone are the most weight-neutral.
- First-generation drugs also cause hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea, sexual dysfunction); among the atypicals, RISPERIDONE does this the most.
- Both classes: avoid alcohol and other CNS depressants, do not drive until the effect is known, space doses evenly, allow SEVERAL WEEKS for full effect, and do not stop abruptly (dizziness, nausea and vomiting, and uncontrolled movements of the mouth, tongue, or jaw). Haloperidol is contraindicated in Parkinson's disease and Lewy body dementia.
| 1st generation (typical) | 2nd generation (atypical) |
|---|
| haloperidol, fluphenazine, chlorpromazine, thiothixene | risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, clozapine |
| HIGH extrapyramidal symptoms and tardive dyskinesia | LOW EPS (risperidone at higher doses is the exception) |
| Higher NMS risk | NMS possible but less common |
| Anticholinergic, sedation, orthostatic hypotension, hyperprolactinemia, photosensitivity | METABOLIC: weight gain, hyperglycemia/new diabetes, hyperlipidemia |
| Better for POSITIVE symptoms (hallucinations, delusions) | Treats positive AND negative symptoms (flat affect, withdrawal, avolition) |
| Cheaper, available as long-acting injections | First-line today; clozapine is reserved for treatment-resistant disease |
| Boxed warning: increased death in elderly with dementia-related psychosis | SAME boxed warning |
Typicals wreck the MOVEMENTS. Atypicals wreck the METABOLISM. Both kill elderly patients with dementia.
What are the pharmacological treatment options for schizophrenia?⭐ HIGH YIELD
SECOND-GENERATION (atypical) antipsychotics are first-line: risperidone, olanzapine, quetiapine, ziprasidone, aripiprazole, paliperidone. First-generation agents (haloperidol, fluphenazine) are alternatives. CLOZAPINE is reserved for TREATMENT-RESISTANT schizophrenia. Long-acting injectables are used when adherence is the problem.
- 'Treatment-resistant' means failure of at least two adequate trials of other antipsychotics. Clozapine is the only drug proven effective there, and it also reduces suicidality, but it requires ANC monitoring for agranulocytosis.
- LONG-ACTING INJECTABLES (LAIs) are given every 2 weeks to every 6 months: risperidone, paliperidone, aripiprazole, haloperidol decanoate, fluphenazine decanoate. They are the answer for repeated relapse from nonadherence.
- It takes SEVERAL WEEKS to see full benefit, and doses should be evenly spaced through the day. Positive symptoms improve first; negative and cognitive symptoms improve slowly if at all.
- For ACUTE agitation, IM haloperidol with lorazepam (with or without diphenhydramine) is common. Long-term, an atypical is preferred.
- Adjuncts: antidepressants for comorbid depression, mood stabilizers for aggression, and benztropine or diphenhydramine to treat EPS. Nonpharmacologic care (case management, family education, supported employment, CBT for psychosis) is part of the plan, not optional.
- Monitor at baseline and on schedule: weight and BMI, fasting glucose and A1C, lipids, blood pressure, AIMS for tardive dyskinesia, and ANC for clozapine. Never stop an antipsychotic abruptly. The textbook adds that patients on lithium AND an antipsychotic must be watched for neurotoxicity (weakness, lethargy, fever, tremulousness, confusion, EPS) and that this should be reported immediately.
Atypical first, clozapine last, long-acting injection when they keep stopping it.
Which medications are indicated for the treatment of both bipolar disorder and seizure⭐ HIGH YIELD
The ANTICONVULSANT MOOD STABILIZERS: VALPROIC ACID/DIVALPROEX, CARBAMAZEPINE, and LAMOTRIGINE. All three treat seizures AND bipolar disorder. (Lithium is a mood stabilizer but is NOT an anticonvulsant.)
- VALPROATE/DIVALPROEX: first-line for acute MANIA and for mixed episodes; also used for generalized, absence, and partial seizures. HEPATOTOXICITY, PANCREATITIS, and TERATOGENICITY (neural tube defects) are boxed warnings. Absolutely avoid in pregnancy. Monitor LFTs, CBC, ammonia, and drug levels (therapeutic 50 to 125 mcg/mL).
- CARBAMAZEPINE: used for bipolar disorder, partial seizures, and trigeminal neuralgia. Boxed warnings for APLASTIC ANEMIA/AGRANULOCYTOSIS and for SJS/TEN, with HLA-B*1502 testing required in patients of Asian ancestry. It AUTO-INDUCES its own metabolism and induces CYP3A4, so it wrecks oral contraceptives, warfarin, and many other drugs. Also causes hyponatremia/SIADH.
- LAMOTRIGINE: best for the DEPRESSED pole of bipolar disorder and for maintenance; also used for partial and generalized seizures. The critical point is the SLOW TITRATION required to avoid STEVENS-JOHNSON SYNDROME. Teach the patient to report ANY rash immediately and never to restart it on their own after a break.
- LITHIUM is the classic mood stabilizer but does NOT treat seizures. Narrow therapeutic index of 0.6 to 1.2 mEq/L; toxicity over 1.5. Maintain consistent sodium and fluid intake; dehydration, low sodium, NSAIDs, ACE inhibitors, and thiazides all raise lithium levels.
- Second-generation antipsychotics (quetiapine, olanzapine, aripiprazole, lurasidone) are also used in bipolar disorder but are not anticonvulsants.
- For any of these, do not stop abruptly: abrupt withdrawal can precipitate seizures or a mood episode.
| Drug | Bipolar role | Seizure role | Biggest danger |
|---|
| Valproic acid / divalproex | Acute mania, mixed episodes | Generalized, absence, partial | Hepatotoxicity, pancreatitis, neural tube defects |
| Carbamazepine | Mania, maintenance | Partial seizures, trigeminal neuralgia | Aplastic anemia/agranulocytosis, SJS/TEN, huge CYP450 induction |
| Lamotrigine | Bipolar DEPRESSION, maintenance | Partial and generalized | STEVENS-JOHNSON SYNDROME - titrate slowly, report any rash |
| Lithium (not an anticonvulsant) | Mania and maintenance; reduces suicide | None | Narrow therapeutic index; toxicity with dehydration, low sodium, NSAIDs |
Valproate, Carbamazepine, Lamotrigine: they calm the seizure AND the mood. Lithium only does the mood.
During general anesthesia, which medications provide sedation and which medications provide🚨 DANGER
SEDATION/hypnosis (unconsciousness and amnesia) comes from PROPOFOL, etomidate, ketamine, midazolam, and the inhaled volatile agents (sevoflurane, desflurane, isoflurane, nitrous oxide). ANALGESIA comes from OPIOIDS: fentanyl, remifentanil, sufentanil, morphine. PARALYSIS comes from NEUROMUSCULAR BLOCKERS: succinylcholine, rocuronium, vecuronium, cisatracurium.
- THE SAFETY POINT: neuromuscular blockers provide NO sedation, NO amnesia, and NO analgesia. A paralyzed patient can be fully awake, in pain, and unable to signal it. Always pair a paralytic with a sedative and an analgesic.
- Propofol is the textbook's example of an IV general anesthetic; it induces anesthesia within about 40 seconds. It causes hypotension and apnea and has NO analgesic properties, so opioids are still required.
- The textbook's three categories of anesthesia: LOCAL (lidocaine injected at the site; EMLA cream is lidocaine plus prilocaine used before IV starts, especially in children), CONSCIOUS SEDATION (midazolam for relaxation plus fentanyl for pain, patient awake and breathing, used for colonoscopy), and GENERAL ANESTHESIA (medication-induced reversible unconsciousness with loss of protective reflexes, requiring airway control).
- Nursing role across all of it: monitor respiratory rate, depth, quality, and SpO2, level of consciousness, and pain, before, during, and after.
- Reversal agents: naloxone for opioids, flumazenil for benzodiazepines, neostigmine with glycopyrrolate or sugammadex for non-depolarizing paralytics. Succinylcholine has NO reversal agent.
- Ketamine is the outlier: it provides sedation AND analgesia AND amnesia while largely preserving airway reflexes and respiratory drive. Malignant hyperthermia is triggered by the volatile inhaled agents and by succinylcholine. Propofol, ketamine, opioids, benzodiazepines, nitrous oxide, and rocuronium are safe alternatives.
| Purpose | Drugs | Note |
|---|
| Sedation / hypnosis / amnesia | propofol, etomidate, midazolam, ketamine, sevoflurane, isoflurane, desflurane, nitrous oxide | Propofol and etomidate give NO pain relief |
| Analgesia | fentanyl, remifentanil, sufentanil, morphine, hydromorphone; ketamine; local anesthetics | Opioids give no amnesia |
| Paralysis | succinylcholine (depolarizing); rocuronium, vecuronium, cisatracurium (non-depolarizing) | NO sedation, NO amnesia, NO analgesia - never give alone |
Sleep, pain, and paralysis are three separate jobs and three separate drugs. Never paralyze someone who is awake.
💉 AlprazolamHIGH ALERTBLACK BOX
Antianxiety, Benzodiazepine (short/intermediate acting)
What it is for
Anxiety, panic disorders with or without agoraphobia, anxiety with depressive symptoms
How it works
Depresses subcortical levels of CNS, including limbic system, reticular formation, may be mediated by GABA
Watch for
CNS: Dizziness, drowsiness, confusion, headache, stimulation, poor coordination, suicide EENT: Blurred vision GI: Constipation, dry mouth, nausea, vomiting, anorexia, diarrhea, weight gain/loss GU: Decreased libido INTEG: Rash, dermatitis
Teaching
- Not to double doses; to take exactly as prescribed; if dose is missed, take within 1 hr as scheduled; that product may be taken with food
- Not to use for everyday stress or for more than 4 mo unless directed by prescriber; not to take more than prescribed amount; that product may be habit forming; that memor …
- To avoid OTC preparations unless approved by prescriber, not to use with grapefruit juice
- Not to discontinue medication abruptly after long-term use
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 AtomoxetineBLACK BOX
Psychotherapeutic—miscellaneous (ADHD), Selective norepinephrine reuptake inhibitor
What it is for
Attention-deficit/hyperactivity disorder
How it works
Selective norepinephrine reuptake inhibitor; may inhibit the presynaptic norepinephrine transporter
Watch for
CNS: Insomnia, dizziness, irritability, crying, mood swings, fatigue, lethargy, paresthesia, suicidal ideation CV: Palpitations, hot flushes, tachycardia, increased B/P, palpitations, orthostatic hypotension, QT prolongation GI: Dyspepsia, nausea, anorexia, dry mouth, weight loss, vomiting …
Teaching
- To avoid OTC preparations, other medications, herbs, supplements unless approved by prescriber; no tapering needed when discontinuing product
- To avoid alcohol ingestion
- To avoid hazardous activities until stabilized on medication
- To get needed rest; patients will feel more tired at end of day; not to take dose late in day, insomnia may occur
🔗 Full card in the drug guide
💉 BuspironeHIGH ALERT
Antianxiety, sedative, Azaspirodecanedione
What it is for
Generalized anxiety disorders
How it works
Acts by inhibiting the action of serotonin (5-HT); has shown little potential for abuse; a good choice with substance abuse
Watch for
CNS: Dizziness, headache, stimulation, insomnia, nervousness, numbness, paresthesia, incoordination CV: Tachycardia, palpitations, hypo/hypertension, chest pain EENT: Sore throat, tinnitus, blurred vision, nasal congestion …
Teaching
- That product may be taken consistently with/without food
- To avoid OTC products, alcohol ingestion, other psychotropic medications unless approved by prescriber; to avoid large amounts of grapefruit juice
- To avoid activities that require alertness because drowsiness may occur
- Not to discontinue medication abruptly after long-term use; if dose is missed, do not double
🔗 Full card in the drug guide
💉 CarbamazepineBLACK BOX
Anticonvulsant, Iminostilbene derivative
What it is for
Tonic-clonic, complex-partial, mixed seizures; trigeminal neuralgia; bipolar disorder
How it works
Exact mechanism unknown; appears to decrease polysynaptic responses and block posttetanic potentiation
Watch for
CNS: Drowsiness, dizziness, fatigue, headache, suicidal thoughts/behaviors CV: Hypertension, AV block, hypotension EENT: Dry mouth, blurred vision, diplopia, nystagmus ENDO: SIADH (geriatric patients) GI: Nausea, anorexia, increased hepatic enzymes, pancreatitis, hepatotoxicity GU: Retention …
Teaching
- To carry emergency ID stating patient’s name, products taken, condition, prescriber’s name, and phone number
- To avoid driving, other activities that require alertness usually for the first 3 days of treatment; dizziness, drowsiness may occur
- Not to discontinue medication quickly after long-term use; seizures may occur
- To immediately report chills, rash, light-colored stools, dark urine, yellowing of skin and eyes, abdominal pain, sore throat, mouth ulcers, bruising, blurred vision, diz …
🔗 Full card in the drug guide
Clozapine – monitoring🚨 DANGER
Clozapine requires ABSOLUTE NEUTROPHIL COUNT (ANC) monitoring because of the risk of AGRANULOCYTOSIS. Baseline ANC must be 1500/mm3 or higher (1000 or higher for benign ethnic neutropenia), then WEEKLY for 6 months, EVERY 2 WEEKS for the next 6 months, and MONTHLY thereafter for as long as the drug is taken.
- Any fever, sore throat, flu-like symptoms, or mouth ulcers on clozapine means CHECK THE ANC NOW. Teach the patient to report these immediately and never to 'wait and see.'
- Clozapine has FIVE boxed warnings: severe NEUTROPENIA, ORTHOSTATIC HYPOTENSION with bradycardia and syncope, SEIZURES (dose-related), MYOCARDITIS and cardiomyopathy, and increased mortality in elderly patients with dementia-related psychosis.
- SEVERE CONSTIPATION and paralytic ileus can be FATAL and are underappreciated. Assess bowel function at every visit and start a bowel regimen.
- Other monitoring: weight, BMI, fasting glucose and A1C, lipids (it causes the worst metabolic effects of any antipsychotic), blood pressure and pulse with dose titration, and troponin/CRP/echo if myocarditis is suspected (usually in the first 4 to 8 weeks).
- Hypersalivation (sialorrhea) is common and paradoxical for an anticholinergic drug; it is worst at night. Also sedation, tachycardia, and dose-related seizures.
- If the drug is interrupted for 48 hours or more, it must be RETITRATED from a low dose, because tolerance to the hypotension is lost quickly. Note: the FDA eliminated the Clozapine REMS program in February 2025, so the centralized registry no longer exists. The ANC monitoring schedule remains in the drug labeling and is still the standard of care and the exam answer.
| Time on clozapine | ANC monitoring frequency |
|---|
| Before the first dose | Baseline ANC must be 1500/mm3 or higher (1000 or higher if benign ethnic neutropenia) |
| First 6 months | WEEKLY |
| Months 6 to 12 | Every 2 WEEKS |
| After 12 months | MONTHLY, indefinitely |
No blood count, no clozapine. Weekly, biweekly, monthly. Fever or sore throat = check the ANC today.
💉 DiazepamHIGH ALERTBLACK BOX
Antianxiety, anticonvulsant, skeletal muscle relaxant, central acting, Benzodiazepine, lon
What it is for
Anxiety, acute alcohol withdrawal, adjunct for seizure disorders; preoperatively as a relaxant for skeletal muscle relaxation; rectally for acute repetitive seizures
How it works
Potentiates the actions of GABA, especially in the limbic system, reticular formation; enhances presympathetic inhibition, inhibits spinal polysynaptic afferent paths
Watch for
CNS: Dizziness, drowsiness, headache, hangover, slurred speech, paradoxical excitation CV: Hypotension, tachycardia EENT: Blurred vision GI: Constipation, nausea, vomiting, diarrhea, weight gain INTEG: Rash, dermatitis, itching, phlebitis (IV) …
Teaching
- That product may be taken with food
- That product not to be used for everyday stress or for >4 mo unless directed by prescriber; to take no more than prescribed amount; that product may be habit forming, rev …
- To avoid OTC preparations unless approved by prescriber
- To avoid driving, activities that require alertness; drowsiness may occur
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 FluoxetineBLACK BOX
Antidepressant, SSRI (selective serotonin reuptake inhibitor)
What it is for
Major depressive disorder, obsessive-compulsive disorder (OCD), bulimia nervosa, premenstrual dysphoric disorder (PMDD), panic disorder Unlabeled: Binge eating disorder, body dysmorphic disorder, fibromyalgia, generalized anxiety disorder …
How it works
Inhibits CNS neuron uptake of serotonin but not of norepinephrine
Watch for
CNS: Headache, nervousness, insomnia, drowsiness, anxiety, tremor, dizziness, fatigue, sedation, poor concentration, abnormal dreams, agitation, seizures, apathy, euphoria, hallucinations, delusions, psychosis, suicidal ideation, neuroleptic malignant syndrome–like reactions CV: Hot flashes …
Teaching
- That therapeutic effect may take 1-4 wk, not to discontinue abruptly, that follow-up will be required
- To use caution when driving, performing other activities requiring alertness because of drowsiness, dizziness, blurred vision
- To avoid alcohol, other CNS depressants
- To notify prescriber if pregnant, planning to become pregnant, or breastfeeding
🔗 Full card in the drug guide
💉 Gabapentin
Anticonvulsant, GABA analogue
What it is for
Adjunct treatment of partial seizures, with/without generalization in patients >12 yr; adjunct for partial seizures in children 3-12 yr, postherpetic neuralgia, primary restless leg syndrome in adults, ALS, neuropathic pain
How it works
Mechanism unknown; may increase seizure threshold; structurally similar to GABA but does not bind to GABAa or GABAb; gabapentin binding sites in neocortex, hippocampus
Watch for
CNS: Dizziness, fatigue, somnolence, ataxia, amnesia, abnormal thinking, depression; children 3-12 yr old, emotional lability, aggression, thought disorder, hyperkinesia, hostility CV: Vasodilation, peripheral edema EENT: Dry mouth, blurred vision, diplopia, nystagmus …
Teaching
- To carry emergency ID stating patient’s name, products taken, condition, prescriber’s name and phone number
- To avoid driving, other activities that require alertness until response is known because dizziness, drowsiness may occur
- Not to discontinue medication quickly after long-term use; to taper over ≥1 wk because withdrawal-precipitated seizures may occur; not to double doses if dose is missed; …
- To report changes in vision, diplopia, eye irritation to provider
🔗 Full card in the drug guide
Ketamine⭐ HIGH YIELD
Ketamine is a DISSOCIATIVE anesthetic that blocks NMDA receptors. Unlike other anesthetics it provides sedation, ANALGESIA, and amnesia while largely PRESERVING airway reflexes, spontaneous respiration, and blood pressure. Used for procedural sedation, induction in hypotensive or asthmatic patients, refractory pain, and (as esketamine) treatment-resistant depression.
- EMERGENCE REACTIONS are the signature adverse effect: vivid unpleasant dreams, hallucinations, delirium, and agitation as the patient wakes up. Reduce them by recovering the patient in a QUIET, DIMLY LIT room with minimal stimulation and tactile contact, and by pretreating or treating with a benzodiazepine (midazolam).
- It INCREASES heart rate, blood pressure, and cardiac output (sympathomimetic), which makes it valuable in shock and hypotension but a poor choice in uncontrolled hypertension, aortic dissection, or severe coronary disease.
- It is a BRONCHODILATOR, so it is the induction agent of choice in status asthmaticus.
- Causes hypersalivation (an antisialagogue such as glycopyrrolate may be given), nystagmus, and increased intraocular pressure. It is one of the SAFE agents in malignant hyperthermia risk.
- Esketamine (Spravato) is an intranasal formulation for treatment-resistant depression and depression with acute suicidality. It carries a REMS: it must be given in a certified health care setting with 2 HOURS of observation, and the patient cannot drive for the rest of the day.
- Ketamine is a Schedule III controlled substance with abuse potential ('Special K'). Chronic misuse causes cystitis and cognitive impairment. Count and waste it per policy.
Ketamine: keeps the airway, keeps the pressure, keeps the pain away. Wake them up in a dark quiet room.
💉 LamotrigineBLACK BOX
Anticonvulsant—miscellaneous, Phenyltriazine
What it is for
Adjunct for the treatment of partial, tonic-clonic seizures; children with Lennox-Gastaut syndrome, bipolar disorder
How it works
Inhibits voltage-sensitive sodium channels, thus decreasing seizures
Watch for
CNS: Dizziness, ataxia, headache, fever, insomnia, tremor, depression, anxiety, suicidal ideation, seizures, poor concentration EENT: Nystagmus, diplopia, blurred vision GI: Nausea, vomiting, anorexia, abdominal pain, hepatotoxicity GU: Dysmenorrhea HEMA: Anemia, DIC, leukopenia …
Teaching
- To take PO doses divided, with or after meals to decrease adverse effects; not to discontinue product abruptly because seizures may occur
- To avoid hazardous activities until stabilized on product
- To carry emergency ID; to notify prescriber of skin rash, increased seizure activity; to use sunscreen, protective clothing if photosensitivity occurs
🔗 Full card in the drug guide
💉 Lidocaine (What are the signs/symptoms of toxicity?)HIGH ALERT
Antidysrhythmic (Class Ib), Aminoacyl amide
What it is for
Ventricular tachycardia, ventricular dysrhythmias during cardiac surgery, digoxin toxicity, cardiac catheterization Unlabeled: Attenuation of intracranial pressure increased during intubation/endotracheal tube suctioning
How it works
Increases electrical stimulation threshold of ventricle, His-Purkinje system, which stabilizes cardiac membrane, decreases automaticity
Watch for
CNS: Headache, dizziness, involuntary movement, confusion, tremor, drowsiness, euphoria, seizures, shivering CV: Hypotension, bradycardia, heart block, CV collapse, arrest EENT: Tinnitus, blurred vision GI: Nausea, vomiting, anorexia HEMA: Methemoglobinemia INTEG: Rash, urticaria, edema, swelling …
Teaching
- About the use of automatic lidocaine injection device if ordered for personal use
- To report signs of toxicity immediately
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 Lithium (What are the signs/symptoms of toxicity? What are the monitoring requirements?)BLACK BOX
Mood stabilizer, Alkali metal ion salt
What it is for
Bipolar disorders (manic phase), prevention of bipolar manicdepressive psychosis
How it works
May alter sodium, potassium ion transport across cell membrane in nerve, muscle cells; may balance biogenic amines of norepinephrine, serotonin in CNS areas involved in emotional responses
Watch for
CNS: Headache, drowsiness, dizziness, tremors, twitching, ataxia, seizure, slurred speech, restlessness, confusion, stupor, memory loss, clonic movements, fatigue CV: Hypotension, ECG changes, dysrhythmias, circulatory collapse, edema, Brugada syndrome, QT prolongation EENT: Tinnitus …
Teaching
- About the symptoms of minor toxicity: vomiting, diarrhea, poor coordination, fine motor tremors, weakness, lassitude; major toxicity: coarse tremors, severe thirst, tinni …
- To monitor urine specific gravity, emphasize need for follow-up care to determine lithium levels; to monitor lithium levels to ensure effective levels and treatment
- Not to operate machinery until lithium levels are stable
- To use emergency ID with diagnosis, product used
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 MethylphenidateBLACK BOX
Cerebral stimulant, Piperidine derivative
What it is for
Attention deficit disorder (ADD), attention-deficit/hyperactivity disorder (ADHD); narcolepsy (except Concerta, Metadate CD, Ritalin LA)
How it works
Increases release of norepinephrine, DOPamine in cerebral cortex to reticular activating system; exact action not known
Watch for
CNS: Hyperactivity, insomnia, restlessness, talkativeness, dizziness, drowsiness, toxic psychosis, headache, akathisia, dyskinesia, masking or worsening of Tourette’s syndrome, seizures, hallucinations, malignant neuroleptic syndrome, aggression …
Teaching
- To decrease caffeine consumption (coffee, tea, cola, chocolate); may increase irritability, stimulation; not to use guarana, yerba maté, cola nut
- To avoid OTC preparations unless approved by prescriber
- To always use dosing dispenser provided for oral suspension dose
- To taper off product over several weeks because depression, increased sleeping, lethargy will occur
🔗 Full card in the drug guide
💉 Phenelzine (What dietary restrictions should the client follow?)BLACK BOX
Antidepressant, Monoamine oxidase inhibitor (MAOI)
What it is for
Depression that has not responded to other antidepressants; described on the label as atypical, nonendogenous or neurotic depression. It is a later-line drug, not a first choice.
How it works
Blocks monoamine oxidase — the enzyme that breaks down serotonin, norepinephrine and dopamine — IRREVERSIBLY and non-selectively. It destroys the enzyme rather than just occupying it, so the body has to build new enzyme before normal breakdown resumes.
Watch for
CNS: Dizziness, drowsiness, insomnia, tremor, hyperreflexia, toxic delirium. CV: Orthostatic hypotension in ordinary use — and a dangerous pressure SPIKE in hypertensive crisis. Edema. GI: Nausea, constipation, weight gain. GU: Sexual dysfunction, urinary retention.
Teaching
- TYRAMINE IS THE ONE TO KNOW. Aged cheese, cured or smoked meat, pickled herring, liver, yogurt, meat or yeast extracts, sauerkraut, soy sauce, draft and craft beer, red wine, and any protein food that has been left out or stored badly. Tyramine plus an MAOI causes a hypertensive crisis.
- Non-alcoholic beer and wine are NOT a safe substitute — the label restricts those too.
- The food and drug rules continue for TWO FULL WEEKS after the last dose. The enzyme was destroyed, not merely blocked, and the body has to rebuild it.
- Hypertensive crisis: a sudden OCCIPITAL headache that may spread forward, stiff or sore neck, palpitations, sweating, nausea and vomiting, dilated pupils, light sensitivity, chest pain. The pulse may be FAST OR SLOW — do not rule it out because the heart rate is low. Emergency.
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 Phenytoin (What are the signs/symptoms of toxicity?)BLACK BOX
Anticonvulsant; antidysrhythmic (IB), Hydantoin
What it is for
Generalized tonic-clonic seizures; status epilepticus; nonepileptic seizures associated with Reye’s syndrome or after head trauma; complex partial seizures Unlabeled: Digoxin toxicity; seizures, prophylaxis in head trauma, subarachnoid hemorrhage
How it works
Inhibits spread of seizure activity in motor cortex by altering ion transport; increases AV conduction
Watch for
CNS: Dizziness, insomnia, paresthesias, depression, suicidal tendencies, aggression, headache, confusion, slurred speech, peripheral neuropathy CV: Hypotension, ventricular fibrillation, bradycardia, cardiac arrest EENT: Nystagmus, diplopia, blurred vision ENDO: Diabetes insipidus GI: Nausea …
Teaching
- That, if diabetic, blood glucose should be monitored
- That urine may turn pink
- Not to discontinue product abruptly because seizures may occur
- Oral hygiene: about the proper brushing of teeth using a soft toothbrush, flossing to prevent gingival hyperplasia; about the need to see dentist frequently
🔗 Full card in the drug guide
💉 Pregabalin
Anticonvulsant, γ-Aminobutyric acid (GABA) analog
What it is for
Neuropathic pain associated with spinal cord injury/diabetic peripheral neuropathy, partial-onset seizures, postherpetic neuralgia, fibromyalgia
How it works
Binds to high-voltage–gated calcium channels in CNS tissues; this may lead to anticonvulsant action similar to the inhibitory neurotransmitter GABA; anxiolytic, analgesic, and antiepileptic properties
Watch for
CNS: Dizziness, drowsiness abnormal thinking, suicidal ideation EENT: Dry mouth, blurred vision, sinusitis GI: Constipation, abdominal pain, weight gain, nausea, vomiting, increased appetite GU: Gynecomastia HEMA: Thrombocytopenia MS: Back pain, rhabdomyolysis, myopathy OTHER: Pruritus …
Teaching
- To carry emergency ID stating patient’s name, products taken, condition, prescriber’s name and phone number
- To avoid driving, other activities that require alertness because dizziness, drowsiness may occur, to obtain clearance from provider if driving is acceptable
- Not to discontinue medication quickly after long-term use; to taper over ≥1 wk; that withdrawal-precipitated seizures may occur; not to double doses if dose is missed, to …
- To notify prescriber if pregnancy is planned or suspected; to avoid breastfeeding
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 PropofolHIGH ALERT
General anesthesia, Phenol derivative
What it is for
Induction or maintenance of anesthesia as part of balanced anesthetic technique; sedation in mechanically ventilated patients
How it works
Produces dose-dependent CNS depression by activation of GABA receptor, hypnotic
Watch for
CNS: Involuntary movement, headache, fever, dizziness, shivering, abnormal dreams, euphoria, fatigue CV: Bradycardia, hypotension, hypertension GI: Nausea, vomiting, abdominal cramping, dry mouth GU: Urine retention, green urine, phlebitis, hives, burning/stinging at inj site, rash RESP: Apnea …
Teaching
- That product will cause dizziness, drowsiness, sedation; to avoid hazardous activities until drug effect wears off
- That drug may cause burning sensation during administration
Antidote / reversal: 1
🔗 Full card in the drug guide
Risperidone & olanzapine⭐ HIGH YIELD
Both are SECOND-GENERATION (atypical) antipsychotics that block D2 and serotonin-2 receptors. RISPERIDONE causes the most EPS and the most HYPERPROLACTINEMIA of the atypicals. OLANZAPINE causes the most WEIGHT GAIN and metabolic syndrome. Both carry the boxed warning for increased mortality in elderly patients with dementia-related psychosis.
- RISPERIDONE is the textbook's prototype atypical: indicated for schizophrenia, acute manic episodes, and irritability associated with autism. At doses above about 6 mg/day it starts behaving like a first-generation drug, with real EPS.
- Risperidone's hyperprolactinemia causes GALACTORRHEA, GYNECOMASTIA, AMENORRHEA, sexual dysfunction, and long-term bone loss. Ask about these directly; patients will not bring them up.
- OLANZAPINE is the metabolic worst case: substantial weight gain, new-onset diabetes, and hyperlipidemia. Monitor weight and BMI, waist circumference, fasting glucose and A1C, and lipids at baseline and on schedule. It is also strongly sedating and anticholinergic.
- IM olanzapine plus IM benzodiazepine should be separated by at least 1 hour because of excessive sedation and cardiorespiratory depression. Olanzapine pamoate (the long-acting injection) requires 3 hours of observation for post-injection delirium/sedation syndrome.
- Both: agranulocytosis is possible, NMS is possible, both cause orthostatic hypotension and falls, both need several weeks for full effect, and neither should be stopped abruptly.
- Both are available as LONG-ACTING INJECTIONS for patients who relapse from nonadherence. Teach both: no alcohol, no driving until the effect is known, evenly spaced doses, rise slowly, and report fever with rigidity (NMS) or any abnormal involuntary movements (tardive dyskinesia).
| Risperidone | Olanzapine |
|---|
| Most EPS of the atypicals, especially above 6 mg/day | Very low EPS |
| Highest PROLACTIN elevation: galactorrhea, gynecomastia, amenorrhea | Little prolactin effect |
| Moderate weight gain | GREATEST weight gain and metabolic syndrome of any atypical |
| Schizophrenia, acute mania, irritability in autism | Schizophrenia, bipolar mania, agitation; also used as an antiemetic |
| Less sedating | Strongly sedating and anticholinergic |
RisperiDONE moves you (EPS and prolactin). OlanZAPine ZAPs your metabolism (weight and sugar).
💉 Valproic acid (What are the monitoring requirements?)BLACK BOX
Anticonvulsant, vascular headache suppressant, Carboxylic acid derivative
What it is for
Simple (petit mal), complex (petit mal), absence, mixed seizures; manic episodes associated with bipolar disorder, prophylaxis of migraine, adjunct for schizophrenia, tardive dyskinesia, aggression in children with ADHD, organic brain syndrome, mania …
How it works
Increases levels of γ-aminobutyric acid (GABA) in the brain, which decreases seizure activity
Watch for
CNS: Sedation, drowsiness, dizziness, headache, depression, behavioral changes, tremors, aggression, weakness, coma, suicidal ideation, hypothermia CV: Peripheral edema EENT: Visual disturbances, taste perversion GI: Nausea, vomiting, constipation, diarrhea, dyspepsia, anorexia, pancreatitis …
Teaching
- To avoid driving, other activities that require alertness
- To drink plenty of fluids
- To discuss with health care professional all OTC, Rx, herbals, supplements taken
- Not to discontinue medication quickly after long-term use, seizures may result; to take as directed; not to skip, double doses; not to chew capsules; to take with milk to …
🔗 Full card in the drug guide
💉 VenlafaxineBLACK BOX
Antidepressant—SNRI, SNRI
What it is for
Prevention/treatment of major depression; depression at the end of life; long-term treatment of general anxiety disorder, panic disorder, social anxiety disorder (Effexor XR only) Unlabeled: Vasomotor symptoms in menopause, andropause, fibromyalgia
How it works
Potent inhibitor of neuronal serotonin and norepinephrine uptake, weak inhibitor of dopamine; no muscarinic, histaminergic, or α-adrenergic receptors in vitro
Watch for
CNS: Emotional lability, dizziness, weakness, headache, hallucinations, insomnia, anxiety, suicidal ideation in children/adolescents, seizures, neuroleptic malignant syndrome–like reaction, anxiety, abnormal dreams, paresthesia CV: Hypertension, chest pain, tachycardia, change in QTc interval …
Teaching
- To notify prescriber of rash, hives, allergic reactions, bleeding
- To use with caution when driving, performing other activities requiring alertness because of drowsiness, dizziness, blurred vision
Antidote / reversal: 1
🔗 Full card in the drug guide
💉 ZolpidemHIGH ALERTBLACK BOX
Hypnotic, Imidazopyridine
What it is for
Insomnia, short-term treatment
How it works
Produces CNS depression at limbic, thalamic, hypothalamic levels of CNS; may be mediated by neurotransmitter γ-aminobutyric acid (GABA), not a benzodiazepine …
Watch for
CNS: Headache, lethargy, drowsiness, daytime sedation, dizziness, confusion, lightheadedness, anxiety, irritability, amnesia, poor coordination, complex sleep-related reactions (sleep driving, sleep eating), depression, somnolence, suicidal ideation …
Teaching
- That dependence is possible after long-term use
Antidote / reversal: 1
🔗 Full card in the drug guide
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Where this came from. Drug cards are pulled from your own drug guide, which was fact-checked against FDA labeling. The concept answers were written for this guide from your course textbook,
Pharmacology (WTCS, 2e), so they should match your lectures. Check anything that contradicts what your instructor said — they write the exam.