Pharm-Drugs (Exam 3)
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| Acetylcholine | NT, metabolized quickly so not therapeutically useful, nonspecific (activate N & M receptors), little CV effects, increase GI motility, stimulate bladder, miosis, bronchoconstriction, increase glandular secretions
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| Epinephrine | NT, increase HR, CX, CO, reflex bradycardia, bronchodilation, dec. GI motility, dec. intraocular pressure
TX: asthma, anaphylaxis, cardiac arrest
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| Norepinephrine | NT, inc. HR, CX, CO, reflex bradycardia, inc. renin in kidney
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| Dopamine | NT, inc. HR, CX, CO, inc. renin in kidney
TX: shock caused by dec. CO and dec. renal function, parkinson's, CHF
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| Seratonin | NT?
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| Amphetamine | indirect symphathomimetic (displace NE from vesicles), competitively inhibits NE reuptake, inhibits MAO activity -> NE lingers
TX: narcolepsy
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| Tyramine | indirect symphathomimetic/sympathetic modulator (alpha-1, beta-1)- cheese, beer, wine; compete with NET
contraind. in pts taking MAOI: incr. HR, CX, CO (reflex bradycardia), initial potentiates NE effects, then depletes NE, inc. renin release in kidney
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| Ephedrine | symp modulator-displaces NE from vesicles, compet. inhib NE reuptake, inhib MAO -> NE lingers (acts like amphetamine)
USES: bronchial relax (beta-2) and mydriasis w/o cycloplegia (alpha-1), used as bronchodilator, eye exams, nasal decong., VASOSPASM
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| Reserpine | sympathetic modulator, binds VMAT-2 irreversibly inhibits vesicular conc. of NE and DA -> SNS depletion
TX: HTN-gradual decline in BP and HR, long duration action
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| Guanethidine | sympathetic modulator, depletes NE in SNS (does not cross BBB), acts like reserpine, false NT
TX: severe hypertension
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| Phenylephrine | alpha-1 selective (receptor agonist)-reflex bradycardia
TX: nasal decongestant
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| Clonidine | alpha-2 selective (receptor agonist)- decrease SNS outflow, decrease BP
TX: hypertension
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| Alpha Methyldopa | alpha-2 selective (receptor agonist)-competitive inhibitor of DOPA decarboxylase -> deplete terminals of DA and NE
TX: HTN during pregnancy
SEs: hepatotoxicity, autoimmune hemolytic anemia
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| Phentolamine | alpha antagonist (nonselective)-dec. BP progressively, hypotension, miosis, nasal congestion, inhibit ejacuation, acts similar to phenoxybenzamine
TX: short-term control of BP and manage pheochromocytoma
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| Phenoxybenzamine | alpha antagonist (nonselective)-increase SNS outflow, reflex tachycardia, dec vasocx, biphasic: comp. blockade of alpha receptors followed by a non-comp. block that is irreversible
TX: pheochromocytoma
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| Doxazosin | alpha-1 antagonist-highly selective a-1 blocker but non-selec. for alpha subtypes, long half-life and long duration of action
TX: HTN and BPH
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| Prazosin | alpha-1 antagonist-reflex tachycardia, decrease vasocx, smooth muscle RX, binds alpha-1 glycoprotein, inc. dose slowly
TX: HTN and BPH, CHF
SEs: syncope
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| Alfuzosin | alpha-1 antagonist-selective for alpha-1A in urinary tract
TX: BPH
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| Tamsulosin | alpha-1 antagonist (alpha-1A, 1D)-reflex tachycardia, dec. vasocx, lower incidence of orthostatic HTN
TX: BPH
SEs: weakness (muscle or psychogenic)
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| Terazosin | alpha-1 antagonist-little first pass metabolism, low tachycardia
TX: HTN, CHF
SEs: syncope
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| Yohimbine | alpha-2 antagonist-inc. HR and BP, no clinical uses
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| Isoproterenol | beta agonist (nonselective)-powerful bronchodilator but not drug of choice due to cardiac effects
SEs: tachycardia, palpitations, headache, flushing
TX: emergencies to stimualate HR in pts with bradycardia or heart block
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| Dobutamine | alpha-1 & beta-1 agonist (mostly beta-1)-increase cardiac efficiency, HR, CX, CO, incr. DBP and SBP, incr. renin secretion
TX: decompensated heart failure
SEs: tachycardia, arrythmias
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| Albuterol | beta 2 agonist-bronchodilation, short acting acute relief, nebulizer
TX: bronchospasm
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| Metaproterenol | beta 2 agonist-bronchodilation, medium duration (oral administration)
TX: bronchospasm, obstructive airway disease
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| Terbutaline | beta 2 agonist-bronchodilation, minimal tachycardia
TX: obstructive airway disease
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| Salmeterol | beta 2 agonist (long-acting)-slow acting, bronchodilation, must be accompanied by steriod for nebulizer
TX: bronchospasm
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| Formoterol | beta 2 agonist (long-acting)-fast acting, bronchodilation, highly lipophilic
TX: bronchospasm
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| Propanolol | beta antagonist (nonselective)-dec. HR, CX, CO; dec. SBP, bronchocx, dec. renin secretion, lipid soluble, fast acting, short half life, first pass effect
TX: HTN and migrane, stage anxiety (low dose)
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| Pindolol | beta antagonist (nonselective)-partial agonist (ISA)
TX: HTN in pts with bradycardia or exercise intolerance
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| Carvedilol | beta antagonist (nonselective beta, alpha-1 blocker), short half-life, no ISA, extensively metabolized by P450
TX: CHF
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| Labetalol | beta antagonist (nonselective beta, alpha-1 blocker)-dec. HR, CX, CO; dec. SBP, bronchocx, dec. renin secretion, ISA at beta-2 receptor
TX: HTN and HTN emergencies
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| Acebutolol | beta-1 antagonist (cardio selective), partial agonist (ISA), dec. HR, CX, CO
TX: HTN, arrythmias, for pts with bradycardia and exercise intolerance
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| Metoprolol | beta-1 antagonist (cardio selective), moderate lipid solubility, first pass effect
TX: HTN
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| Atenolol | beta-1 antagonist (cardio selective)-dec. HR, CX, CO; dec. SBP, long-lasting, specific, reduced CNS activity, no bronchocx, dec. renin secretion, long half-life
TX: HTN w/o bronchocx
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| Bisoprolol | beta-1 antagonist (cardio selective)-well tolerated, no ISA activity, long half-life
TX: std. when combined with ACE inhibitor and diuretic -> HTN
SEs: bradycardia
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| Esmolol | beta-1 antagonist (cardio selective), very short half-life
TX: admin. IV where immediate onset of blockade is required
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| Bethanechol | muscarinic agonist-
TX: enhance intestinal activity and promote urination, reduced CV SEs compared to carbachol or methacholine, more selective (M3 in GI and bladder)
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| Pilocarpine | muscarinic agonist-similar to synthetic agents with similar SE and no receptor selectivity
TX: first choice for open angle glaucoma (topical)
SEs: impaired night vision, spasms of accommodation
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| Carbachol (Carbamylcholine) | muscarinic agonist
TX: open angle glaucoma, useful alternative when resistance to pilocarpine or physostigmine
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| Atropine | muscarinic antagonist-brady (low), inc. HR (normal) vasocx, bronchodl, dec GI motiliy, urine retention, mydriasis
TX: GI spasms, eye exams, CHEI toxicity, anethesic adjuvant, motion sickness, overactive bladder, ulcer, anti-parkinsonism
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| Scopolamine | muscarinic antagonist-brady (low), incr. HR (normal), vasocx, bronchodl, dec gastric motility, urine retention, mydriasis
TX: GI spasms, eye exams, CHEI toxicity, anethesic adj, motion sickness, overactive bladder, ulcer, anti-parkinson
SEs: CNS effec
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| Pirezepine | muscarinic antagonist (M1)-
TX: used with H-2 blockers to reduce gastric acid secretions to produce gastric ulcer healing
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| Ipratropium | muscarinic antagonist, decreased bronchial secretions, bronchocx
TX: COPD
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| Tiotropium | muscarinic antagonist-bronchial effects similar to tiptropium, administered as an inhalant, long duration of action (24h)
TX: asthma, COPD
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| Tubocararine | competitive NMJ blocker-inc. HR, dec. BP, resp. paralysis, bronchocx
DI: aminoglycosides and tetracyclines
CONTRA: asthma, MG
TX: procedures that require muscle paralysis
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| Atracurium | competitive NMJ blocker-?
TX: procedures that require muscle paralysis
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| Mivacurium | competitive NMJ blocker-more bronchocx, inc. histamine release, short duration of action, dec. cardiac effects (less tachycardia)
CONTRA: asthma, compromised pulmonary fx
TX: procedures that require muscle paralysis
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| Vecuronium | competitive NMJ blocker-inc. cardiac effects (more tachycardia), dec. histamine release (less bronchocx)
TX: procedures that require muscle paralysis
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| Succinylcholine | depolarizing NMJ blocker-dec. HR, inc. BP, resp. paralysis, slight histamine release
DI: w/ halothane (abnormal ryanodine receptor) -> malignant hyperpyrexia
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| Botulinum toxin | ACh release inhibitor (irreversible)-cleaves synaptobrevin and SNAP to prevent vesicle fusion/release
TX: dystonias, spasticity, stroke, chronic anal fissure, severe wrinkles, spasmodic dysphonia, hyperhydrosis
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| Neostigmine | AChE inhibitor (reversible)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression
TX: paralytic ileus, tx of MG, xerostomia
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| Physostigmine | AChE inhibitor (reversible)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression
TX: atropine toxicity (crosses BBB)
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| Edrophonium | AChE inhibitor (reversible)-very short acting
TX: diagnosis of MG, PAT
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| Diisopropyl flurophosphate (DFP) | AChE inhibitor (irreversible, organophosphate)-reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression, volatile, lipid soluble, cross BBB
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| Nerve Gases (Soman) | AChE inhibitor (irreversible, organophosphate)--reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression
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| Echothiphate | AChE inhibitor (irreversible, organophosphate)--reflex tachy, vasodilation, bronchocx, inc secretions, inc. GI motility, micturition, miosis, skeletal m. fasiculation, CNS depression
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| 2-pralidoxime (2-PAM) | AchE reactivator-splits covalent bond, forms oxime-phosphonate -> leaves regenerated ChE
TX: reverses CHEI toxicity
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| Dantrolene | skeletal muscle relaxant-binds ryanodine receptor -> prevent Ca2+ release
TX: malignant hyperpyrexia caused by succinylcholine+halothane
SEs: muscle weakness, sedation, hepatitis
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| Nicotine | nicotinic agent-Nm and Nn agonist, can produce depolarization blockade in toxic doses
SEs: respiratory stim leading to arrest, convulsions, nausea
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| Varenicline | partial nicotine receptor agonist selective for alpha4beta2 nicotinic receptor, long half-life
TX: nicotine addiction
SEs: weight gain
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| Teriparatide acetate | synthetic PTH, diagnostic for pseudohypoparathyroidism
MOA: inc extracell and circul. Ca2+
TX: daily intermittent injection for osteoporosis in men and postmen women at high risk of fracture
SEs: may lead to hypercalcemia
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| Calcitonin | MOA: dec. osteoclast-mediated Ca2+ mobilization
TX: severe hypercalcemia (SQ or IM every 12 hrs), osteoporosis (when HRT contraind), paget's disease
SE: nausea, facial flushing, swelling (hands), inflamm rxn, urticaria
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| Calcitriol (Vit D), Dihydrotachysterol | MOA: inc. intestinal Ca2+ uptake, inc. osteoclast different, inc. osteocalcin express.
TX: hypocalcemia, hypoparathyroidism, pseudoparathyroidism, osteoporosis (combo with ca2+), rickets and osteomalacia, impaired vit D synthesis
SE: hypervitaminosis
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| Aledronate, Ibandronate, Zoledronic acid | bisphosphonates
MOA: inhibit bone resorption, may produce gains in bone mass
TX: osteoporosis (dec fracture risk-50%), paget's disease, hypercalcemia assoc with malignancy
SE: hypocalcemia, hypophosphatemia, upper GI irritation
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| Allopurinol | inhibitor of uric acid synthesis-standard txt for chronic tophaceous gout
MOA: comp. inhibitor of xanthine oxidase
SE: maculopapular rash, GI, hepatotoxicity, fever, hypersens.
-not useful for acute gout attacks
-inhibit kidney reperfusion injury
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| Febuxostat | inhibitor of uric acid synthesis, selective inhibitor of xanthine oxidase
-rapidly and extensively absorbed
TX: chronic gout (prophylactic NSAIDs or colchicine used in beg to prevent gout attack)
SE: GI intolerance, hepatic function alterations
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| Probenecid | uricosuric agent-inhibit proximal tubule resorption, oral admin, not used in acute gout attacks
TX: hyperuricemia control
DI: PCN, ASA, sulfa, allopurinol
TOX: GI, dermatitis, nephrotic syndrome
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| Colchicine | gout pain and inflammation
MOA: binds microtub tubulin -> dec. urate phagocytosis
-admin oral
TOX: GI, blood dyscrasias, CNS depression, shock
TX: gouty arthritis attacks, pseudogout, fam. med fever
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| Indomethacin | gout pain and inflammation, anti-inflammatory
TX: acute gouty attacks
-not used for chronic gout or prophylaxis
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| Rasburicane | increases uric acid degradation-lowers uric acid levels better than allopurinol
TX: initial management of pediatric pts with chemo-induced hyperuricemia
SE: prod of antibodies, acute renal failure, anaphalaxis, GI abnormalities
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| Alprazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, short acting
TX: anxiety, depression
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| Chlordiazepoxide | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, rapidly absorbed, short acting
TX: anxiety, alcohol withdrawal
TOX: lots!
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| Clonazepam | benzodiazepines, anti-convulsant-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, long acting
TX: status elipticus
TOX: lots!
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| Diazepam | benzodiazepines, anti-convulsant-rapidly absorbed, long acting
TX: anxiety, status epilepiticus
TOX: lots!
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| Flurazepam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, long acting
TX: insomnia
TOX: lots!
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| Triazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, rapidly absorbed, very short acting
TX: insomnia
TOX: lots!
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| Pentobarbital, Secobarbital | barbituate-act at GABA-A receptor -> prolong Cl channel opening -> inhibition, short-intermediate acting
-drugs of abuse
TOX: excess sed, confusion, lethargy, tolerance, phys/psyh dependence -> WD, respiratory arrest
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| Flumazenil | BZ-1 and BZ-2 receptor antagonist-reverse toxicity caused by benzos and non-benzos, not effective with other agents, short acting, must be given IV
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| Busopirone | alternative anxiolytic-slowly develop anti anx effect without sedation
MOA: no GABA, maybe 5HT1A?
TX: general anx disorder (not panic/PTSD)
-no sedation, dependence, withdrawal, cross tolerance, no muscle relaxation
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| Anti-histamines | may produce some anxiety relief as consequence of sedative properties, useful in pts prone to abuse of benzos
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| Amitriptyline | TCA-inhibit NE and 5-HT reuptake
TX: depression, eunuresis, pain, ADHD
TOX: lots!
SE: pronounced anti-ACh visual effects (mydriasis and dec. accomodation)
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| Nortriptyline | TCA-inhibit NE and 5-HT reptake
TX: depression, eunuresis, pain, ADHD
TOX: lots!
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| Imipramine | TCA-inhibit NE and 5-HT reuptake
TX: depression, eunuresis, pain, ADHD
TOX: lots!
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| Clomipramine | TCA
TX: depression, eunuresis, pain, ADHD, OCD
TOX: lots!
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| Desipramine | TCA-inhibit NE reuptake
TOX: lots! sudden death in children
TX: depression, eunuresis, pain, ADHD
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| Bupropion | cyclic antidepressant-inhibit DA reuptake
TX: depression, nicotine withdrawal
-dec. CV SEs, dec. sexual complications, dec. seizure threshold
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| Mirtazapine | cyclic antidepressant-enhance NE release
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| Trazodone | cyclic antidepressant-heavily promoted, rel. poor AD, few SEs, sedation, good hypnotic
-produces priapism
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| Fluoxetine | SSRI-inhibit 5-HT reuptake
-long acting, active metabolite, inhib p450 system
TX: depression, OCD, bulimia
TOX: lots!-inc risk of suicide
DI: MAOI -> seratonin syndrome
SE: weight loss
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| Sertraline | SSRI-like fluoxetine but less akathesia, no inhib of p450 system, shorter half-life
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| Paroxetine, Fluvoxamine | SSRI-similar to sertraline, some inhib of p450 system (P>F), short half-life
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| Citalopram | SSRI-similar to sertraline, most selective, widely used
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| Duloxetine | SNRI?
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| Venlafaxine | SNRI?
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| Phenelzine | MAOI
TX: depression, narcolepsy, phobia anxiety D/O, OCD
TOX: dec BP, headache, sexual dysfunction, hypertension/hypotension
DI: tyramine->hypertensive crisis
-mood elevation in depressed/normal indiv.
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| Selegiline | MAOI-relatively selective for MAO-B, used in PD, also approved for major depression
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| Midazolam | benzodiazepines-bind a1-gamma1 on GABA-A receptor, dec. neuron activity, sleep dose-response curve, short acting, water soluble
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| Zolpidem | non-benzo BZ1 agonist, short acting
TX: insomnia
TOX: bizarre nighttime behavior, less SEs than benzos/barbs (reversed by flumazenil)
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| Thiopental | barbituates-act at GABA-A receptor -> prolong Cl channel opening -> inhibition, ultra short acting
TX: anesthesia adjunct
TOX: excess sed, confusion, lethargy, tolerance, phys/psyh dependence -> WD, respiratory arrest
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| Ramelteon | melatonin-1 and 2 agonist -> decrease sleep onset
TX: insomnia (sleep onset problems)
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| Lithium | anti-manic-Na+ or Mg2+ replacement -> dec. IP3/DAG, dec. cAMP, dec. NT release, oral absorp, narrow therapeutic window, only drug that dec. suicide
TX: mania
TOX: acute-fatigue, weakness, tremor, chronic-dec thyroid, diabetes insipidus, nephritis, edema
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| Valproate | anti-manic, anti-convulsant-block Na+, enhance GABA, used for early mania, used as lithium adjunct
TX: mania
TOX: sedation, GI, hepatotoxicity, birth defects
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| Carbamazepine | anti-manic, anti-convulsant-block Na+ and enhance GABA, use anti-convulsant dose, used if lithium inadequate
TX: mania
TOX: diplopia, ataxia, GI, aplastic anemia, birth defects, agraunlocytosis
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| Olanzapine | anti-manic-blocks 5HTA>D2>alpha
TX: schizophrenia, schizoaffective disorder, bipolar diorder, mania, tourette's syndrome
TOX: weight gain, metabolic syndrome
-less SEs
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| Aripiprazole | anti-manic-partial agonist at D2 and 5HT2A
TX: schizophrenia, schizoaffective disorder, bipolar diorder, mania, tourette's syndrome
-less SEs, no weight gain
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