Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
104 Cards in this Set
- Front
- Back
Acetazolamide
|
Diamox Carbonic anhydrase inhibitor Site 1 (prox tubule) Block Na+/H+ antiporter; inhibits HCO3- reabsorption & carbonic anhydrase ↓ CSF & intraocular volume Glaucoma, epilepsy, acute mountain sickness Alkalinized Urine --> Hyperchloremic Metabolic acidosis DI with Memantine
|
|
Furosemide
|
Lasix High-ceiling ("Loop") Site 2 (Asc. Limb) Block Na+/K+/2Cl- (NKCC2 transporter); acts on tubular side of cell; effective natriuretic; ↑ renal blood flow Diuresis; vasodilator Edema (acute and/or pulmonary), ↑ Ca2+; HTN in pts w ↓ renal blood flow PO or subq Half-life = 50 min Hypokalemia, ototoxicity, hypochloremic metabolic alkalosis, hyperglycemia, hyperuricemia, hypertriglyceridemia, GI problems, hypomagnesemia, hypotension must be secreted into proximal tubule; counter-current washout; DI w/ COX inhibitors, propranolol, organic acids, albumin binders
|
|
Bumetanide
|
Bumex High-ceiling Site 2 NKCC2 blocker; 4x as potent as furosemide Diabetic pts or pts allergic to furosemide Less hyperglycemia OH DANG!- ototoxicity, hypokalemia, dehydration, allergy (sulfa), nephritis, gout
|
|
Ethacrynic acid
|
Edecrin High-ceiling Site 2 NKCC2 blocker w/o sulfonamide group Pts w/ sulfa allergy More GI problems, less hyperglycemia
|
|
Torsemide
|
Demedex High-ceiling Site 2 NKCC2 blocker w/ 2x greater bioavailability Long half-life (QD dose)
|
|
Chlorothiazide
|
Diuril Thiazide Site 3 (DCT) Block Na+/Cl- cotransport; produce hyperosmolar urine Long-term therapy HTN management, CHF, hypercalciuria, mild edema, diabetes insipidus PO Long half-life, 1-3 weeks for effect ↓ K+ (supplement with K+ diet, salts, or spironolactone); ↓ Na+; hyperuricemia; orthostatic hypotension, ↑ Ca2+, ↑ glucose, hyperlipidemia (may return to normal); hypersensitivity; impaired excretion of Li+; metabolic alkalosis; toxic with digitalis; decrease renal BF Not useful if GFR < 30 ml/min
|
|
Hydrochlorothiazide
|
Hydrodiuril Thiazide Site 3 NCC blocker, more potent than CTZ
|
|
Spironolactone
|
Aldactone K+-sparing Site 4 (Collecting tubule) Aldosterone receptor antagonist (competitive); blocks aldosterone Na+/K+ exchange; inhibits K+ loss Slight Na+ excretion & diuresis K+ protection from diuretics; strong action in CHF or liver cirrhosis, hyperaldosteronism PO with food Slow on/off (steroid action) Hyperkalemia (bad in DM or ↓ GFR); gynecomastia, impotence, menstrual irregularities never with physiological antagonist
|
|
Eplerenone
|
Ispra K+-sparing Site 4 Specific mineralocorticoid receptor antagonist Combo w/ site 3 diuretics HTN, post-MI, K+ protection Hyperkalemia
|
|
Triamterene
|
Dyrenium K+-sparing Site 4 Physiologic antagonist of aldosterone (electrogenic, fast-acting); inhibits Na+ channel influx, dissipates transepithelial potential PO Half-life = 3 hours Rare nephrotoxicity w/ indomethacin
|
|
Amiloride
|
Midamor K+-sparing Site 4 PO Half-life = 6-9 hours hyperkalemia, increased Li reabsorption, elevate urate
|
|
Dopamine
|
Hemodynamic a1, b1, DA receptor agonist ↑ blood flow & GFR, ↓ counter-current exchange Renal vasodilator w/ dobutamine post-MI
|
|
Caffeine
|
Hemodynamic Vasa recta
|
|
Mannitol
|
Osmotic Plasma compartment Countercurrent washout, 4 attributes: inert, osmotically active, filtered not reabsorbed, not metabolized; prevent reabsorption of water Cerebral edema, glaucoma, prophylaxis of acute renal failure IV Excess CSF volume if removed rapidly: HA, nausea, vomiting; contraindicated in anuria, peripheral edema, CHF, & dehydration
|
|
Isosorbide
|
Osmotic Plasma compartment Eye surgery IV or PO
|
|
Propranolol
|
β-blocker Antagonize stretch receptors and ↓ renin release HTN, tremor Ineffective when plasma renin activity is low
|
|
Clonidine
|
"α2-agonist/CNS adrenolytic
" HTN |
|
Methyldopa
|
CNS adrenolytic HTN
|
|
Captopril
|
Capoten PDP (ACE) inhibitor; has sulfhydryl group Block conversion of angiotensin I to II. ↑ Renin release ↓ blood pressure & aldosterone secretion HTN (w/ DM nephropathy), CHF, angina, post-MI PO w/o food Half life= 1.5-2 hours Hypoglycemia w/ insulin (due to sulpher moeity) proteinuria, hypogustia, hypersensitivity, cough, neutropenia; DO NOT use in combination with triamterene or amiloride: hyperkalemia
|
|
Enalapril
|
Vasotec PDP inhibitor; has carboxyl group; prodrug → enalaprilat (active) PO w/ or w/o food; IV enalaprilat Half-life = 11 hours (QD dose) fewer side effects
|
|
Lisinopril
|
Zestril PDP (ACE) inhibitor PO w/ or w/o food Half-life = 12 hours no plasma binding
|
|
Benazepril
|
Lotensin most potent PDP inhibitor
|
|
Losartan K
|
Cozaar Angiotensin II receptor antagonist Blocks binding of angiotensin II to AT-1 receptors Alone or + HCTZ (Hyzaar) PO Half-life of metabolite = 9 hours Dizziness, hyperkalemia excreted in bile
|
|
Valsartan
|
Diovan Angiotensin II receptor antagonist Alone or + HCTZ (Diovan HCT) PO w/o food
|
|
Aliskiren
|
Non-Peptide Renin Inhibitor "Blocks production via the classical pathway of all forms of angiotensins.
" PO poor bioavailability (3%) but long half life Diarrhea, hyperkalemia Does not inhibit kinins |
|
Fludrocortisone
|
Aldosterone agonist Mineralocorticoid Given w/ glucocorticoid Adrenal insufficiency PO
|
|
DOCA (deoxocorticosterone acetate)
|
Aldosterone agonist IV or IM (in oil)
|
|
Spironolactone
|
Aldactone Aldosterone competitive antagonist Binds to mineralocorticoid, androgen & progestin receptors HTN, CHF weakly diuretic
|
|
Eplerenone
|
Inspra Aldosterone competitive antagonist more specific mineralcorticoid agonist HTN, post-MI
|
|
Triamterene
|
Aldosterone physiological antagonist DO NOT use with ACE inhibitors K+ sparing
|
|
Amiloride
|
Aldosterone physiological antagonist
|
|
Allopurinol
|
Zyloprim Xanthine oxidase inhibitor Inhibits biosynthesis of uric acid (competitive antagonist) Long-term therapy Chronic, tophagous gout w/ ↑ urate production, ↓ renal function PO May precipitate gout attack on initiation of therapy; GI sx, skin rash, hypersensitivity; drug interactions Use if hypersensitivity to uricosuric agents
|
|
Febuxostat
|
Uloric Xanthine oxidase inhibitor Inhibits biosynthesis of uric acid (more specific than allopurinol) Reduced frequency of hypersensitivity compared to allopurinol Increased CV adverse effects
|
|
Colchicine
|
Impairs chemotaxis of granulocytes into gouty joints Acute therapy or + probenecid Acute gout attacks Nausea & vomiting Most likely interferes with tubulin activity
|
|
Pegloticase
|
Krystexxa Uricase Recombinant Exogenous enzyme (uricase) oxidizes uric acid to alltoin (highly water soluble) Acute reduction of serum urate Treatment of gout unresponsive to standard therapy IV infusion
|
|
Probenecid
|
Benemid Uricosuric High doses ↑ urate excretion, ↓ urate reabsorption & secretion (competitive inhibition) Long-term therapy Chronic gout or 1-shot treatment of uncomplicated gonococcal + long-acting penicillin (blocks secretion) PO GI problems, kidney stones, hypersensitivity; Low dose: "paradoxical effect" ↓ urate excretion and ↑ plasma urate; aspirin prevents actions on urate; additive actions with sulfinpyrazone; antagonizes diuretics highly lipid soluble; passive reabsorption from nephron
|
|
Sulfinpyrazone
|
Anturane Uricosuric Metabolite of phenylbutazone, strong acid; ↑ urate excretion Chronic gout w/ hypersensitivity to probenecid More GI problems, less hypersensitivity antithrombotic properties of unknown mechanism
|
|
Ethanol
|
alcohol Sedative- hypnotic Binds to GABAa receptor to open Cl- channels; inhibits NMDA glutamate receptors rapidly absorbed by GI; Liver EtOH dehydrogenase or MEOS → aldehyde dehydrogenase → acetate (uses NADH/NADPH) zero-order kinetics: 1 drink(6-8g)/hr Methanol toxicity Disinhibition, CNS depression (ataxia, slurred speech, coma, delirium); risk of aspiration, vasodilation, cardiac depression, diuresis, blackouts Cirrhosis, pancreatitis, PUD, malnutrition, CA, FAS, Wernicke- Korsakoff thymine deficiency (causes neuropathy, confusion) Anxiety, insomnia, anorexia, sympathetic autonomic hyperactivity, delirium tremens, seizures; subsides within 3-7 days OD: supportive, prevent aspiration; Chronic: rehab, thiamine; Withdrawal: BZ for seizure, haldol, clonidine Inhibits metabolism and duration of warfarin and phenytoin; contraindicated with drugs irritating the GI; cross-tolerance w/ benzodiazepines & barbiturates
|
|
Disulfiram
|
Adjunct to treat alcoholism
|
|
Naltrexone
|
Alcoholism
|
|
Acamprosate
|
Alcoholism
|
|
Methanol
|
Blurred vision, blindness, seizures, coma, acidosis Supportive therapy, ethanol Necrosis of bilateral putamina & claustra, toxic to retinal ganglion cells
|
|
Ethylene Glycol
|
renal insufficiency/injury due to metabolic acidosis and oxalate deposition in the kidney. Ethanol, Fomepizole
|
|
Thiopental
|
IV general anesthesia Drowsiness, respiratory depression; induce hepatic δ-aminolevulinic acid synthase (worsen acute intermittent porphyria); add to EtOH CNS depression; ↑ metabolism of steroid hormones (hepatic microsomal enzymes) Cellular & enzymatic tolerance; physical dependence Anxiety, insomnia, anorexia, autonomic hyperactivity (similar to EtOH) Respiratory support, gastric lavage, hemodialysis, osmotic diuretics cross-tolerance w/ other sedative=hypnotics
|
|
Pentobarbital
|
Preanesthesia, regional anesthesia
|
|
Phenobarbital
|
Epilepsy, w/drawal from Sedative-Hypnotics; congenital hyperbilirubin, neonatal jaundice
|
|
Cocaine
|
Topical anesthesia (inherent vasoconstriction) Euphoria, ↑ activity, ↓ appetite, sympathetic stimulation, sexual arousal; insomnia, anxiety, tachycardia, HTN, sexual dysfunction Huge tolerance; anxiety, insomnia, psychological dependence; CVA, seizure, coronary vasospasm, MI, psychosis; nasal perforation, "crack baby" (cocaine) Crash: anxiety, fatigue, hypersomnia, hunger; Withdrawal: drug craving, anhedonia, depression, dysphoria
|
|
Amphetamine
|
ADHD, narcolepsy (+) necrotizing arteritis
|
|
Nicotine
|
Patch, gum, inhalant for nicotine dependence ↑ motor activity, cognitive function, ADH, ↑ BP & HR, GI tract tone; ↓ appetite, N&V CANCER, Cellular, some metabolic tolerance; develops rapidly, long-lasting; psychological dependence ↓ DA in nucleus accumbens; craving, tremor, dizziness, irritability, anxiety, ↑ appetite Nicotine treatments + behavioral therapy; may use antidepressants: Bupropion; Varenicline (nicotine receptor antagonist) It's the smoooooooke..., crosses placenta
|
|
Marijuana/Dronabinol
|
N&V from CA chemo, appetite stimulant in AIDS; ↓ intraocular pressure in glaucoma; neuropathic pain Euphoric state, ↑ appetite, relaxation; tachycardia, red eyes, laughter, inattention, tremulosness, ↓ ST memory Lung damage from smoke; cognitive impairement No demonstrated physical dependence/ withdrawal syndrome
|
|
LSD
|
Dilated pupils, ↑ BP, tachycardia; Good Trip: altered consciousness, euphoria, ↑ sensory awareness, introspection; Bad Trip: anxiety, agitation, panic reactions, psychosis, hallucinations Tolerance, cross-tolerance w/ LSD, psilocybin, mescaline BZ and therapy
|
|
Phencyclidine
|
Euphoria, personality dissociation, poor judgment, aggression, psychosis; hallucinations, seizures, respiratory depression, coma; renal failure, rhabdomyolysis Induced vomiting, respiratory support, seizure control w/ BZ, reduce sensory stimulation
|
|
Hydrochlorothiazide
|
HCTZ Thiazide diuretic ↓ reabsorption of Na+; loss of Cl-, K+, Mg2+, water ↓ vascular volume, ↓ TPR HTN, CHF, hypercalciuria, diabetes insipidus Hypokalemia, hyponatremia, gout, volume depletion First step therapy for prevention of HF
|
|
Furosemide
|
Lasix Loop diuretic Inhibits Na+/K+/Cl- cotransport ↓ vascular volume, ↓ TPR CHF, pulmonary edema (acute, rapid onset) Ototoxicity, hypokalemia, gout, hypovolemia, hypomagnesemia
|
|
Spironolactone
|
Aldosterone competitive antagonist (K+ sparing) K+ retention, Na+ excretion ↓ vascular volume CHF, cirrhosis Hyperkalemia with ACE Inh or ARB; gynecomastia, GI upset, mental confusion
|
|
Eplerenone
|
Aldosterone competitive antagonist (K+ sparing) K+ retention, Na+ excretion ↓ vascular volume CHF, cirrhosis Hyperkalemia with ACE Inh or ARB; gynecomastia, GI upset, mental confusion
|
|
Amiloride
|
Dyrenium K+-sparing Physiologic antagonist of aldosterone (electrogenic, fast-acting); inhibits Na+ channel influx, dissipates transepithelial potential
|
|
Atenolol
|
Tenormin β1-blocker ↓ BP, afterload ↓ CO, ↓ renin activity HTN Less bronchial constriction; careful in CHF, asthma, COPD, and heart block pts QD or BID; longer T1/2 than metoprolol
|
|
Propranolol
|
Inderal β antagonist Equal β1 and β2; blocks NE and Epi blocks cardiostimulatory effects of NE and Epi and thus ↓ cardiac output, blocks β1 renin release and thus angiotensin formation (↓ O2 demand); crosses BBB HTN, arrhythmia, angina, migraine prophylaxis, anxiety, essential tremor reduction Careful in heart failure; blocks B2→worsens asthma, COPD, and emphysema; hypoglycemia; allergy complications; abrupt cessation of B antagonist can precipitate angina and increase risk of sudden death "PO has poor bioavalibility, 3-4 hours (large first-pass effect), competitive antagonist lipophilic & crosses BBB
" |
|
Prazosin
|
Minipress α1 antagonist Blocks vascular α-1 receptors, arterial & venous: blocks NE effects Relax smooth muscle, vasodilation Benign prostatic hypertophy (BPH), mild to moderate HTN; heart failure (↓ pre- and afterload) Orthostatic hypotension, inhibits ejaculation, little reflex tachycardia "3 hour half-life (liver metabolism), not block A2 receptors & does not increase neural release of NE
" |
|
Carvedilol
|
CoReg α1 antagonist, β antagonist *Pan beta (1&2) blocker→decreases cardiac, arterial, and kidney effects of B1&2 actions of NE *alpha 1 blocker→decreases vasoconstriction and BP *antioxidant→counteracts production of O2 radicals CHF Used with ACE inhibitors and diuretics; blocks ischemia, further damage
|
|
Clonidine
|
Catapres alpha 2 agonist prejunctional a2 receptors inhibit release of NE, decreases vasoconstriction through CNS (a2 receptors normally produce vasoconstriction) ↓ BP Hypertension; opioid withdrawal; diarrhea Rebound HTN, hypotension, dry mouth, sedation, should not be abruptly discontinued
|
|
Enalapril
|
Vasotec ACE Inhibitor ↓ BP, afterload increase vasodilation, decrease aldosterone CHF, HTN, MI, angina Cough, orthostatic hypotension, hyperkalemia, not in pregnancy! Cough from failure to inactivate bradykinin
|
|
Losartan
|
Cozaar ARB ↓ BP, afterload increase vasodilation HTN, CHF Orthostatic hypotension; hyperkalemia; not in pregnancy!
|
|
Aliskiren
|
Renin inhibitor Inhibit peptidase activity of renin: Reduce Angiotensin II vasodilation HTN hyperkalemia Same efficacy as ACEs/ARBs, may have greater renin rebound
|
|
Verapamil
|
Calan, Isoptin Ca2+ blocker: diphenylalkylamine Bind to subunit of L-type channel, ↓ Ca2+ influx ↓ vascular tone; ↓ HR (countered by baroreceptor reflex) HTN (mild to severe); angina due to spasm Headache, flushing, constipation, premature labor, peripheral edema; NOT in CHF, heart block, or WPW
|
|
Nifedipine
|
Procardia Ca2+ blocker: dihydropyridine cardiosparing ↓ vascular tone, less heart effect Short or sustained release
|
|
Hydralazine
|
Apresoline Direct arterial relaxants ↓ BP, afterload possible NO donor, mechanism not fully understood HTN, CHF Headache, flushing, slow acetylators: lupus-like syndrome Depends on rate of liver acetylation
|
|
Minoxidil
|
Loniten/Rogaine K+ arterial relaxants ↓ BP, afterload HTN, baldness Headache, flushing, hypertrichosis
|
|
Omalizumab
|
Xolair Anti-IgE antibody binds circulating IgE Long-term control Asthma & Allergic Rhinitis SubQ every 2-4 weeks long-acting not all patients respond to treatment
|
|
Beclomethasone
|
Beclovent, Vaneril; Beconase, Vancenase Corticosteroid Inhibit synthesis of inflammatory mediators Increase number and responsiveness of B2 receptors (relaxation) Emergency or long-term Asthma, Rhinitis Inhalation (chronic) or IV (acute); Topical for Rhinitis Rapid systemic metabolism High lipid solubility; Promotes oropharyngeal candidiasis, dysphonia (hoarseness), suppression of adrenal axis in children, bone loss? First of its class
|
|
Flunisolide
|
AeroBid; Nasalide Asthma, Rhinitis
Corticosteroid |
|
Ciclesonide
|
Corticosteroid
prodrug that is activated by esterases in mucosal cells Asthma, Rhinitis |
|
Budesonide
|
Pulmicort; Rhinocort
Corticosteroid Asthma in young children, Rhinitis Nebulizer |
|
Methylprednisolone
|
Solu-medrol Emergency Asthma IV
|
|
Cromolyn
|
Intal; Nasalcrom, Crolom
Cromone Prevents release of mediators from mast cells Inhibits early and late responses; long-term Asthma: antigen, cold, & exercise induced; Rhinitis Inhalation, prior to exercise; nasal spray, optic solution 4-8 week trial Will not abort an acute attack |
|
Nedocromil
|
Tilade; Alocril Cromone Inhibits mast cell activation & chemotaxis Long-term control; prior to exercise or exposure to known antigen 3-4 days to be efffective
|
|
Zileuton
|
Zyflo Anti-leukotriene 5-lipooxygenase inhibitor Long-term control; attenuates bronchospasm and inflammatory response Asthma, Rhinitis PO Short-acting ↑ liver enzymes; interferes w/ drug metabolism: warfarin, propranolol, theophylline
|
|
Montelukast
|
Singulair Leukotriene receptor antagonist Asthma, Rhinitis PO Long-acting excreted in bile
|
|
Ipratroprium
|
Atrovent Muscarinic antagonist bronchodilatation, reduce secretion long-term control Asthma, intolerant to B agonists; Rhinitis slow onset, long duration local irritation
|
|
Tiotropium
|
Spiriva Muscarinic & Cholinergic antagonist Chronic Bronchitis, emphysema long acting
|
|
Atropine
|
Cholinergic antagonist
|
|
Epinephrine
|
Primatine, Bronkaid α & β-adrenergic agonist inhibit mast cell release, increase mucociliary clearance, relax airway smooth muscle long-term control, PRN for acute symptoms Asthma Inhalation, SubQ (emergency) immediate onset, short duration Vasoconstriction, Cardiac stimulation, skeletal muscle tremor; refractoriness (counteracted w/ corticosteroid); mask progression of disease
|
|
Isoproterenol
|
Isuprel, Medihaler-Iso, Vapolso β- adrenergic agonist Asthma Inhalation, parenterally
|
|
Pirbuterol
|
Maxair beta 2 agonist Asthma Inhalation
|
|
Theophylline
|
Methylxanthine Block adenosine receptors, inhibit cAMP phosphodiesterase, alter translocation of intracellular Ca acute & long-term control Asthma, chronic bronchitis, emphysema IV, PO widely variable: disease, drug & diet dependent Headache, insomnia, anxiety, behavioral & learning problems, N&V, heartburn, ulcers, tremor, convulsions, arrhythmias; very narrow TI good oral bioavailability; crosses BBB, placenta
|
|
Diphenhydramine
|
Benadryl Ethanolamine "First Gen" H1 receptor antagonist, muscarinic receptor antagonist Rhinitis, sedation, motion sickness, common cold prophylaxis PO onset within 30 min., max effect at 1-2 hrs, duration 3-6hrs Sedation, anti-cholinergic action, hypersensitivity, tolerance, CNS stimulation in children Cross BBB & placenta
|
|
Chlorpheniramine
|
Tavist, Chlor-Trimeton Alkylamine
|
|
Hydroxyzine
|
"First Gen" H1 receptor antagonist, muscarinic receptor antagonist
|
|
Promethazine
|
"First Gen" H1 receptor antagonist, muscarinic receptor antagonist
|
|
Loratadine
|
Claritin "Second Gen" H1 receptor antagonist Longer half life Absorption altered with grapefruit juice; arrhythmias No crossing of the BBB, no sedation, no anticholinergic action
|
|
Desloratidine
|
"Second Gen" H1 receptor antagonist Longer half life Absorption altered with grapefruit juice; arrhythmias No crossing of the BBB, no sedation, no anticholinergic action
|
|
Fexofenadine
|
"Second Gen" H1 receptor antagonist Longer half life Absorption altered with grapefruit juice; arrhythmias No crossing of the BBB, no sedation, no anticholinergic action
|
|
Epinephrine
|
Adrenalin Cl alpha receptor agonist Vasoconstriction Rhinitis Topical rapid onset Few systemic; rebound congestion, rhinitis medicamentosa, tachyphylaxis
|
|
Phenylephrine
|
alpha receptor agonist Vasoconstriction Rhinitis Topical rapid onset Few systemic; rebound congestion, rhinitis medicamentosa, tachyphylaxis
|
|
Pseudoephedrine
|
Sudafed, Afrinol PO slow onset, longer acting dizziness, tremor, insomnia, irritability, palpitations, HTN less potential for dependence
|
|
Codeine
|
Antitussive Opiod analgesic decreases sensitivity of cough center antitussive action at doses lower than those required for analgesia
|
|
Dextromethorphan
|
Pertussin Antitussive
Opiod sterioisomer decreases sensitivity of cough center no analgesic or addictive effect |
|
Guaifenesin
|
Expectorant stimulate secretory activity, reduce viscosity of mucus Triggers vagal reflex - near emetic doses required
|
|
Terpin hydrate
|
Expectorant
|
|
Iodides
|
Expectorant
|
|
Acetylcysteine
|
Mucomyst reduces sputum viscosity Inhalation
|
|
Chlorpromazine
|
Thorazine Aliphatic Phenothiazine (PTZ) Low Antagonist at dopamine D2 receptors, mostly in mesolimbic & mesocortical tracts (therapeutic effect); also antagonize histamine H1-receptors (CNS), muscarinic cholinergic receptors (PNS), and α-adrenergic receptors (PNS) Schizophrenia, Schizoaffective Disorder, Mania, Tourette's syndrome, antiemetic (except thioridazine), Delusional disorder; Depression w/ psychotic features, Borderline Personality Disorder, severe agitation/violence, delirium, dementia SE's: Agranulocytosis, cholestatic jaundice, photosensitivity Impotence/sexual dysfunction, orthostatic hypotension (α-adrenergic blockade); sedation, weight gain (histamine H1 blockade); anticholinergic crisis; seizures, hyperprolactinemia; withdrawal-like syndrome (nausea, vomiting, insomnia, headache); neuroleptic malignant syndrome Additive: CNS depressants (sedative- hypnotics, alcohol), Levodopa, anticholinergics; antacids decrease absorption, TCAs reduce blood levels, smoking increases metabolism; macrolide antibiotics Improves positive symptoms
|
|
Thioridazine
|
Mellaril Antagonist at dopamine D2 receptors, mostly in mesolimbic & mesocortical tracts (therapeutic effect); also antagonize histamine H1-receptors (CNS), muscarinic cholinergic receptors (PNS), and α-adrenergic receptors (PNS)
Piperidine PTZ Low SE's: ↑ Q-T interval, arrhythmia, priapism, retrograde ejaculation Cardiotoxic - sudden death; retinal pigmentation and blindness Hydroxyzine potentiates toxicity |