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Definition
Muscarinic agonist used for rx of closed angle glaucoma bc causes miosis |
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Muscarinic blocker, used for dilating pupils for eye exams |
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ChE inhibitor used for closed angle glaucoma bc of miosis Tertiary amine (preferable bc easily crosses membranes) |
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carbonic anhydrase inhibitor that is used for open angle glaucoma bc decreases aqueous formation |
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Beta blocker (B1=B2) that inhibits epinephrine release which reduces aqueous; may cause asthma attacks |
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Beta blocker (B1 > B2) --> inhibits E release --> reduces aqueous; safer for asthmatics than timolol |
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Alpha 2 agonst that decreases aqueous & increases uveoscleral aqueous outflow |
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PGE2 analog that increases uveoscleral output. Side effects are longer eyelashes & discolored iris |
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Blocks tryptophan hydroxylase |
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Blocks VMAT --> Depletes 5HT, NE (used to treat depression) |
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indirect agonist that releases 5HT --> acts on all receptors |
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used for cataplexy (narcolepsy) but build up tolerance & decreases delta sleep |
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antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension) |
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antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension) |
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antidepressant - sedative that helps w sleep in already depressed pts (downside = hypotension) |
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Definition
sedative but has anticholinergic side effects |
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benzodiazepine w/ little-no REM suppression or rebound, long acting |
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benzodiazepine w/ little-no REM suppression; intermediate acting but slow onset & possible rebound insomnia |
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shortest acting benzodiazepine - has REM suppression, anterograde amnesia, rebound insomnia |
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BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset Side effects: drowsiness, headache, N/D/Dizziness |
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BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset & ultra-short acting (t1/2 = 1 hr) - good for sleep initiation problems Side effects: memory problems |
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BZD1 receptor - safer than benzos, doesn't affect sleep stages, has a quick onset, intermed acting (t1/2 = 6 hr); efficacy >6 mos |
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Melatonin receptor agonists |
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Definition
short acting, reduce sleep latency, and work by acting thru suprachiasmatic nucleus; but inconsistent results / no regulation |
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anti-seizure for complex partial seizures |
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anti-seizure for complex partial seizures |
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Anti-convulsant / anti-seizure for absence generalized seizures |
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TCA; inhibits presynaptic NT reuptake (NE, 5HT, DA) Effective & inexpensive AE's: sedation (H1 blocker), orthostatic hypotension, dizziness (alpha-1 blockade), dry mouth & constipation (cholinergic blockade) |
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SSRI; inhibits presynaptic 5HT reuptake Approved for >8 yrs old AE's: N/D, sexual side effects, insomnia, headache |
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MAOI; inhibits breakdown of NT Effective & cheap AE's: dizziness, orthostatic hypotension (a1 blockade), insomnia; do not mix w tyramine (red wine, cheese); fatal if combined w SSRI |
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Definition
aka wellbutrin; dopamine reuptake inhibition; used for depression No weight gain or sexual side effects AE's: insomnia, GI, lower seizure threshold |
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aka Remeron; 5HT2 antagonist --> increases 5HT + a2 antagonist --> increase NE; used for depression AE's: weight gain, sedation |
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NT stabilizer; inhibits NE & DA + enhances 5HT used for tx of bipolar; AE's: intentional tremor, weight gain, polyuria Takes 1-3 weeks for onset and has interactions w/ caffeine & iburpofen |
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Anticonvulsant also used for bipolar (mixed mania/rapid cycling); increasese GABA quick onset AE's: weight gain, sedation |
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GABA-A agonist that increases the frequency of Cl- channel opening Anxiolytic - used for GAD, situational anxiety, panic disorder, general anesthesia AE's: CNS depression, impaired judgment, anterograde amnesia, respiratory depression |
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Barbiturate; GABA-A agonist |
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GABA-A & glycine inhibitor (non-competitive); Toxicity = tonic clonic seizures used for barbiturate poisoning |
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Convulsant; GABA-A antagonist |
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gamma hydroxybutyrate (GHB) |
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Definition
breakdown product of GABA that causes coma, seizures, vomiting, depression, amnesia |
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Glycine receptor antagonist; convulsant Does NOT act on GABA! Treat OD w/ CNS depressant (diazepam) |
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Indirect acting sympathomimetic Blocks NET (uptake 1) --> increases NE & DA Sx = mydriasis, tachycardia, htn, hyperthermia (from vasoconstriction) Can be used in nasal surgery (good vasoconstriction) |
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Indirect acting sympathomimetic Blocks NET (uptake 1) + stimulates NE release --> increases NE Sx = arousal, euphoria, vasoconstriction (reduces congestion), tachycardia (B1 > reflex bradycardia) |
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Found in red wine & cheese; displaces NE from synaptic vesicles --> increases NE release Tyramine + amphetamine = depletion of NE Tyramine + MAOI = way too much NE |
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D1 receptor agonist; used to treat hypertension by stimulating vasodilation |
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a1, B1, B2 agonis; B2 > a1 --> decrease diastolic bp (but no change in overall BP), HR increases (B1 - no reflex bc no BP change) |
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alpha1 agonist; used for nasal decongestion, hypotension. Side effect = mydriasis |
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a1, B1, B2 agonist; a1 > B2 --> increase diastolic BP |
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a1, B1 agonist --> increase BP; HR decreases (reflex) |
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B1 = B2; decrease diastolic BP (B2), increase systolic = (very small decrease in overall BP); HR increases (B1); used for Rx of arrhythmias |
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a2 agonist --> decreases NE; used for nicotine addiction, opiate addiction, benzo addiction (reduces sympathetic side effects of withdrawal) |
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B1 agonist - increases HR |
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B2 agonist - bronchodilation + vasodilation (decrease in BP) |
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a1 blocker - used to treat BPH; side effect = hypotension |
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a1 blocker (some a2) - used to treat pheochromocytoma (adrenal hyperplasia = increase E release) |
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B1 = B2 blocker; decreases BP (but not good for asthmatics); NO reflex tachycardia |
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B1 selective blocker; decreases BP + NO reflex tachycardia |
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Definition
a1, B1, B2 blocker; decreases BP; NO reflex tachycardia |
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Definition
a1, a2 blocker; used to treat erectile dysfunction --> vasodilation in penis |
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Definition
GABA-A agonist (inhibits adenosine reuptake); causes paradoxical excitation (via disinhibition); used for trigeminal neuralgia, poison ivy, methanol poisoning; AE's: ataxia, resp depression, diuresis, gastric acid secrtion |
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Definition
Prolongs GABA Cl- channel opening; used for mild sedation, anticonvulsant, anxiolytic, sleep |
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Blocks tuberomammillary H projections; blocks H1 --> mild sedation |
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acts on receptors in suprachiasmatic nucleus --> cause mild sedation; used for rx of insomnia |
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Blocks acetaldehyde dehydrogenase (enzyme in breakdown of alcohol); used for alcohol rehab bc causes really bad hangover effects if any alcohol is had |
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5HT1a autoceptor agonist / 5HT2/7 blockade - after 4-6 wks downregulates autoceptor (increase 5HT); anxiolytic & mild sedative; does not interact w/ alcohol For Rx of GAD (equally effective to benzos) |
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5HT2/7 blockade --> increases slow wave sleep |
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Tx of personality disorder; calming & anxiety reduction Benzo |
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Benzo used as an anticonvulsant |
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Benzo w/ longer half-life |
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Benzo Used for personality disorder tx |
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SSRI + SNRI; inhibits reuptake + downregulates |
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Used for treatment of benzo overdose |
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Pentylenetetrazole (metrazole) |
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Definition
GABA receptor antagonist --> convulsant Used to activate EEG for diagnosing siezure d/o |
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Xanthines (Caffeine, theophylline, theobromine) |
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Definition
Blockade of adenosine A1 & A2 recptors --> increase Ca++ --> increase cAMP Clinical use = prolonged episodes of apnea in preemies Effect: alert, nervous, convulsions (v high doses); bronchial muscle relaxation, diuretic, increases HR Toxicity = PVCs, delirium, emesis |
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Xanthine, clinical use = bronchodilation |
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Definition
racemic amphetamine; stimulates NE (&DA) release and blocks reuptake Clinical use: narcolepsy, ADHD, obesity Effects: sympathomimetic, increase BP & reflex bradycardia |
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Definition
D isomer amphetamine stimulates NE (&DA) release and blocks reuptake Clinical use: narcolepsy, ADHD, obesity Effects: sympathomimetic, increase BP & reflex bradycardia |
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Definition
Amphetamine but with fewer peripheral effects; stimulates NE (&DA) release and blocks reuptake Clinical use: narcolepsy, ADHD, obesity Effects: sympathomimetic, increase BP & reflex bradycardia |
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aka Ritalin; sympathomimetic used to treat ADHD |
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sympathomimetic used as an alertness-enhancing drug |
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Definition
Binds nicotinic receptors, increases DA in nuc accumbens Used in early alzheimer's Effects = alertness, euphoria, muscle relaxation, appetite reduction, increased HR & BP, GI motility Treat addictions w Clonidine, buproprion, varenicline |
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Definition
Carotid K+ channel blocker --> increased DA release Effects = respiratory stimulation Use = COPD, anesthesia recovery Treat OD w/ short-acting barbiturate |
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Definition
binds to kainate receptor (more so than glutamate) |
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Definition
competes with Mg2+ on NMDA (glutamate) receptor --> blocks receptor --> hallucinations, delusions, cognitive deficits |
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Definition
endogenous cannabinoids - act on CB1 receptor in CNS & CB2 in periphery Effects = anxiety, insomnia, depression, sperm morphology, birth defects, impaired attention |
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Definition
Endogenous opioids made in hypothalamus & pituitary (POMC); bind to mu & Delta |
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Endogenous opioids found in CNS, adrenal, enterics; synthesized by preproenkephalin bind to mu & delta |
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Endogenous opioid - in CNS & spinal cord especially; synthesized by preprodynorphin Kappa (and weak mu) agonist |
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Opioid agonist used for severe pain Given parenterally long duration |
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Orally effective opioid, but less potent than morphine Good antitussive synergystic effect w/ aspirin |
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opioid; Crosses BBB --> strong CNS effect High abuse potential |
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opioid oral efficacy + long duration (not as much withdrawal) used for treating opioid addictions |
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Opioid (demerol) : less potent than morphine; orally effective.. But NO antitussive, constipation, miosis Good for acute pain / labor |
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very potent opioid; short duration used for anesthesia no histamine release |
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opioid (darvon) - similar to codeine but lower efficacy (banned by FDA) |
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mixed opioid agonst/antagonist more potent than morphine - parenteral or nasal spray Psychotomimetic side effects |
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mixed opioid agonst/antagonist less potent than morphine can cause increase in BP (but has less respiratory depression) |
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mixed opioid agonist/antagonist that is long acting, with slow dissociation from mu receptor --> decrease efficacy + long acting = very effective in treating opiate dependence |
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Opioid does not cross BBB; used as a anti-diarrheal |
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Opioid, but also blocks NMDA receptor --> good antitussive but no analgesia or respiratory depressoin |
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opioid antagonist short half life, parenteral Good for opiate overdose (cheapest) |
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opioid antagonist long half life + oral bioavailability = good for treating opiate addictions (in highly motivated ppl); also used to treat alcohol addiction |
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opioid antagonist longer half-life than naloxone, but still parenterally given (probably preferable to naloxone in treating heroin overdose, but much more $$$) |
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Definition
typical, low-potency antipsychotic Blocks D2-4, 5HT2A, alpha1, M, H1 Used for acute psychosis, psychosis w/ positive symptoms side effects = anticholindergic, neuroleptic malignant syndrome (but low EPS) |
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typical, low-potency antipsychotic Blocks D2 side effects = prlonged QT interval |
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typical, hi-potency antipsychotic D2-4 block Acute antipsychotic side effects = EPS, lactation, sedation, Tardive |
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Definition
typical, hi-potency antipsychotic D2-4 block Acute antipsychotic side effects = EPS, lactation, sedation, Tardive |
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Definition
Atypical antipsychotic D4 block (also 5HT2A, alpha1, M, H1) side effects = seizures, paradoxical salivation, anticholinergic effects, sedation |
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Definition
Atypical antipsychotic 5HT2A > D2-D4, a1, H1, M block Used for negaive symptoms, bipolar mania side effects = weight gain, diabetes, anticholinergic; don't use in elderly |
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Atypical antipsychotic 5HT2A > D2-D4, a1, H1, M block Best for elderly side effects = postural hypotension, weight gain, agitation |
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Used for MS treatment --> downregulates TH1, upregulate Tregs Reduces relapse > interferons |
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Interferon Beta 1a (Avonex, REBIF) |
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Definition
For MS treatment Reduces relapse rate, development of new lesions, lesion growth Side effects = psych, seizures, hepatitis, cardiomyopathy, autoimmune 30% develop neutralizing antibody |
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Interferon Beta 1b (Betaseron) |
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Definition
For MS treatment similar to beta 1a, but questionalbe duration & significance of benefit May develop neutralizing antibodies |
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Mitoxantrone (Novantrone) |
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Definition
For MS treatment Reduces attack rate, slows disease progression IV only, can cause local tissue damage, potentially fatal CHF may occur - very cardiotoxic |
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Definition
MAB therapy for MS Effective in reducing attacks & new MRI lesions (no long-term data) 1/300 risk of PML if + for JCV |
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Sphingosine 1-phosphate receptor modulator, treatment for MS First line oral therapy, produces lymphopenia in the brain? Side effects = many |
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Definition
Short-term benefit for MS treatment Good rx for acute attacks by restoring BBB |
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