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Transcript
PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 DRUG TYPE THERAPEUTIC USE ADVERSE EFFECT ANYTHING ELSE CHOLINERGIC AGONISTS(bronchoconstriction, bradycardia, hypotension, miosis, blur vision, urinary incontinence, INC secretions) Pilocarpine Physostigmine® (Estrine) Neostigmine® (Prostigmine) Pyridostigmine® (Mestinon, Regonol) Edrophonium® (Tensilon) Ecothiophate® (Phospholine) Tacrine® (Cognex) Donepezil (Aricept®) Rivastigmine (Exelon®) Galantamine (Razadyne®) Direct acting Indirectacting Indirectacting Indirect acting -Topically in eye for glaucoma Blurred vision -P.O for xerostomia -Topically in eye for glaucoma Blurred vision -I.V for anticholinergic poisoning -P.O and S.C. for mysathenia gravis -P.O and I.V. for mysathenia gravis Indirect acting Indirect acting Indirectacting Indirectacting -Used to diagnose mysathenia gravis -Topically for glaucoma Indirect acting Indirectacting -P.O for Alzheimer’s disease -Not used as much anymore for Alzheimer’s disease -P.O for Alzheimer’s disease -mild to moderate Alzheimer’s disease and dementia Has lactone group-subject to hydrolysis Intermediate acting; 3° amine-can enter CNS Intermediate acting; 4° amine-no CNS activity Intermediate acting; has pyridine ring; 4° amine Short acting; has phenol group; subject to MAO Long acting (organophosphate) Liver toxicity DOA=1.5-4 hrs. P-450 Inhibits theophylline met N&v, anorexia, 5mg/day10 mg/day bronchoconstriction DOA=70-104hrs. P-450 sweating metabolism DOA=1.4-1.7hrs. Low level of hepatoxicity Dual action; no hepatoxicity 1 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 Pralidoxime Achase -Used for organophosphate ® (Protopam ) inhibitor poisoining (2-PAM) ANTICHOLINERGICS(bronchodilation, tachycardia, constipation, hallucinations, urinary retention, blur vision, DEC secretions) Atropine AntiChol -I.V for bradycardia esp. one Irritability, restless, “atropine flush” associated with MI delirium Contraindicated in -Organophosphate poisoning glaucoma Scopolamine AntiChol -motion sickness Drowsy, delirium, hallucinations Transderm Scop AntiChol -Topically for motion sickness Dry mouth, drowsiness Tropicamide AntiChol -Eye examination to cause Photophobia ® (Mydriacyl ) mydriasis Cyclopentolate AntiChol -Eye examination to cause Photophobia ® (Cyclogyl ) mydriasis Datura AntiChol -Used to be used for COPD Tertiary amine; doesn’t stay strauonium long in bronchioles Ipratropium AntiChol -FDA for COPD 4X a day; Quart. amine ® (Atrovent ) -Off-label for asthma Tiotropium AntiChol -FDA for COPD 1Xa day; Quart. amine; ® (Spiriva ) -Off-label for asthma poorly absorbed Dicyclomine AntiChol -P.O for peptic ulcer Tertiary amine ® (Bentyl ) -P.O. for diarrhea Propantheline AntiChol -P.O for peptic ulcer Quart. amine ® (Probanthine ) -P.O. for diarrhea 2 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 Tolterodine (Detrol®) Trospium (Sanctura®) Fesoterodine (Toviaz®) Oxybutynin (Ditropan®) Darifenacin (Enablex®) Solifenacin (Vesicare®) AntiChol -P.O for urinary incontinence AntiChol -P.O for urinary incontinence AntiChol -P.O for urinary incontinence AntiChol -P.O for urinary incontinence AntiChol -P.O for urinary incontinence AntiChol -P.O for urinary incontinence Constipation, dry mouth, blurred vision Constipation, dry mouth, blurred vision Constipation, dry mouth, blurred vision Constipation, dry mouth, blurred vision Constipation, dry mouth, blurred vision Constipation, dry mouth, blurred vision 2mg BID 5mg TID 7.5mg Q.D.(once a day) 5mg Q.D.(once a day) ADRENERGIC AGONISTS DRUG RECEPTOR USES EFFECTS OR OTHER FACTS α1, α2, β1, β2, Inhalation I.V, S.C for asthma; β-1=↑ contractility=↑ systolic Epinephrine ® β3 Agonist Topical hemostatic; Prolongs β-2=vasodilation=↓ diastolic (Adrenaline ) Norepinephrine (Levophed®) α1, α2, β1 agonist and little bit of β2, β3 Isoproterenol (Isuprel®) β1, β2, β3 Agonist; nonselective β local anesthesia; Reversing Cardiac arrest(Intracardiac) LOW DOSES: ↑ systolic and ↓ diastolic so ↑ in HR( somewhat β-1) HIGH DOSES: ↑diastolic and ↓ HR(both α1) I.V. for certain hypotensive states Anti-hypertensive Inhalation for asthma but not so much anymore β-1=↑ contractility=↑ systolic α-1=vasoconstiction=↑ diastolic Compensatory reflex bradycardia ↓ HR β-1=↑ contractility=↑ systolic β-2=vasodilation=↓ diastolic(more potent than Epi because no α affects) 3 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 Dopamine (Intropin) Dobutamine (Dobutrex ® injection form) α -1 agonists D1, β1, α1 Agonist Phenylephrine (NeoSynephrine®) Naphozoline (Privine®, Naphcon®) I.V. for shock ↑ in renal blood flow without ↑BP; at high doses, stimulates β-1 on heart; met by COMT and MAO (-)= α-1 agonist; (+)=α-2 antagonist. Both=β-1 agonists; (+) is more potent than (-) isomer. Decongestant(nasal + eye) HAVE IMIDAZOLINE RING; 2arylakylimidazoline; decongestants α1 Agonist; selective α-1 agonist Topical Decongestant (nasal and eye); topical mydriatic; I.V. for pressor effect(α-1) α-1=vasoconstriction=↑ systolic and diastolic pressures; Reflex bradycardia=↓ HR; stop use after 3 days to avoid rebound congestion; no COMT metabolism α-1 agonist Topically for eye decongestion One time use; for chemical and allergic conjuctivitis limited access to CNS; has imidazoline ring Topically for eye decongestion Topically for nasal decongestion Topically for nasal decongestion Anti-hypertensive; skeletal muscle relaxant; treats glaucoma; sedation Glaucoma(used topically) Hypotension/sedation Skeletal muscle relaxant One time use; for chemical and allergic conjuctivitis limited access to CNS; has imidazoline ring No more than 3 days to avoid rebound congestion; limited access to CNS; imidazoline ring No more than 3 days to avoid rebound congestion; limited access to CNS; imidazoline ring Dual α and β agonist Tetrahydrozoline α-1 agonist (Visine®) Oxymetazoline α-1 agonist ® (Afrin ) Xymetazoline α-1 agonist ® (Octrivin ) α-2 agonists Brimonidine (Alphagan®) Tizanidine α-2 selective α-2 agonist Nitrogen instead of carbon at center Works on spinal cord 4 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 (Zanaflex®) Dexmedtomidin e (Precedex®) β-2 selective α-2 agonist Terbutaline (Brethine®) Metaproterenol (Metaprel®) Albuterol (Proventil®, ProAir®) Levalbuterol (Xopenex®) Pirbuterol (Maxair®) β2 selective agonist Salmeterol (Serevant®) β2 selective agonist Formoterol (Foradil®) β2 selective agonist Arformoterol β2 selective β2 selective agonist β2 selective agonist β2 selective agonist I.V. for sedation and anesthetic adjunct Asthma; prevent premature labor Little or no respiratory depressant; used in ICUs Nervousness, insomnia, palpitations or tremors, tachycardia, headache, angina pectoris P.O., S.C., inhalation for Metabolized by glucouronidation; lasts 4-6 hrs; asthma can be given p.o(no COMT); chronic and acute use P.O, inhalation for asthma Same Isoproterenol but –OH in meta position which means no COMT; glucourodination P.O, inhalation for asthma Metabolized by glucouronidation; lasts 4-6 hrs; chronic and acute use; has S(bronchial contraction) and R isomer; no COMT/MAO Inhalation for Asthma Pure R isomer-take fewer for same effect; less side effects; no COMT/MAO Inhalation for asthma Metabolized by glucouronidation; lasts 4-6 hrs; can be given orally(no COMT/MAO); chronic and acute use; Chronic attacks of asthma LABAs; DOA>12 hrs; only used for chronic use; for prevention can cause inflammation in bronchial tissues Slow onset and dissociation; long DOA; no COMT Chronic attacks of asthma LABAs; DOA>12 hrs; only used for chronic use; for prevention can cause inflammation in bronchial tissues; formal aminobeta directing; no COMT/MAO; long DOA; racemic(R,R) (S,S) stereochemistry Chronic attacks of asthma R,R enantiomer of Formoterol so high potency 5 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 (Brovana®) agonist Advair β2 selective agonist β2 selective agonist β2 selective agonist β2 selective Symbicort Dulera Ritodrine (Yutapar®) Chronic attacks of asthma at low dose; no COMT; ↑ risk of asthma deaths; has formal aminobeta directing Combination LABA: Salmeterol + Fluticasone Chronic attacks of asthma Combination LABA: Formoterol + Budesonide Chronic attacks of asthma Combination LABA: Formoterol +Momesonide I.V., and P.O to prevent premature labor Indirect-Acting Appetite suppression, narcolepsy, ADHD Amphetamine Indirect-acting Appetite suppression, ® (Adderall ) narcolepsy, ADHD Methamphetamine Both indirect and direct(β-2) Appetite suppression, narcolepsy, ADHD Methylphenidate Indirect-acting P.O. for Narcolepsy, (Ritalin®) ADHD Ephedrine Indirect-acting Pseudoephedrine Indirect-acting P.O for decongestion Dextroamphetamine Promote release of/inhibit reuptake of NE; non-catecholamines; more lipid solubleCNS ↑BP, ↓HR(reflex bradycardia), at higher doses, cause ↑HR because reflex bradycardia is overriden and individual experiences tachycardia; Racemic mixture; (S) isomer has fewer side effects than (R) Phenylisopropylamines Indirect-acting Threo(high priority groups on opposite sides) is 400X as potent as erythro(on same side) Racemic mixture-more side effects than pure; Phenylisopropylamines Can be converted to methamphetamine; L(+) isomer; (S, S) pure isomer=less side effects (S) isomer only meaning fewer side effects; 6 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 (Dexedrine®) Modafinil (Provigil®) Armodafinil (Nuvigil®) Fenoldopam (Corlopam®) Indirect-acting Txt of sleep and narcolepsy Indirect-acting Promoting wakefulness Indirect-acting Anti-hypertensive 10X as potent as R enantiomer CNS stimulant; atypical α-1 NE stimulant; R-S racemate R enantiomer Benzodiazepine derivative; moderate affinity for α2 receptors ADRENERGIC BLOCKERS Selective α-1 blockers Prazosin (Minipress®) Doxazosin (Cardura®) Terazosin (Hytrin®) Quinazolines Selective α-1 blockers Selective αblockers Selective α-1 blockers Selective α-1 blockers Alfuzosin (Uroxatral®) Tamsulosin (Flomax®) Non-selective α blockers Phenoxybenzamine Non-selective α (Dibenzyline ®) blockers Phentolamine Non-selective α blockers Non-sel β blocker Hypertension 2-3X a day; disadvantage to HBP txt HBP + BPH 1x a day Quinazolines HBP 1X a day Quinazolines ONLY for BPH; 1X a day Quinazolines Quinazolines BPH(lower incidence of orthostatic hypertension) Control BP in pheochromocytoma Control BP in pheochromocytoma Hypertension, glaucoma Blocks α-2 release of NE; Tachcardia; Orthostatic hypotension; also causes miosis and nasal stuffiness Pheochromocytoma=benign tumor of adrenal glands; NE and Epi ↑BP. Not used much anymore Pheochromocytoma=benign tumor of adrenal glands; NE and Epi ↑BP. Not used much anymore Side effects: depression, insomnia, wheezing, bradycardia 7 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 Propranolol (Inderal) Timolol-Timoptic Nadolol (Corgard ®) Carteolol (Cartrol ®) Sotalol (Betaspace ®) Levobunolol (Betagan ®); Metipranolol (Opti-Pranolol ®) Selective β-1 blockers Atenolol (Tenormin) Betaxolol (Betoptic) Metoprolol (Lopressor) Esmolol (Brevibloc) Nebivolol (Bystolic) Non-selective βblocker Non-selective βblocker Non-selective βblocker Non-selective βblocker Non-selective βblocker Non-selective βblockers Selective βblocker Selective βblocker Selective βblocker Selective βblocker Selective βblocker P.O and I.V for HBP -Glaucoma-topically -Hypertension -Topically for open-angle glaucoma Aryloxypropanolamines: Standard Beta blocker; highly lipophiliccleard by liver; non-selective; active metabolite Aryloxypropanolamines Aryloxypropanolamines; one of the longest lasting beta blockers Aryloxypropanolamines Not an aryloxypropanolamine; exception to SAR Other aryloxypropanolamine P.O. for HBP and angina pectoris -Glaucoma P.O. for HBP, CHF, and angina pectoris; I.V. for acute or chronic MI; Extended release for CHF I.V only to treat cardiac arrhythmias Side effects: depression, insomnia, wheezing, bradycardia Aryloxypropanolamines Aryloxypropanolamines Aryloxypropanolamines For cardiac arrhythmias in surgical settings 8 PRINCIPLES OF DRUG ACTION: DRUGS FOR TEST 1 β-blocker with α-1 antagonist activity Labetalol β-blocker with ® (Trandate ) α-1 antagonist activity Carvedilol β-blocker with ® (Coreg ) α-1 antagonist activity P.O for HBP; potentially for orthostatic hypotension(α-1) Extended release for CHF; HBP; Aryloxypropanolamines; selective α-1 blocker; nonselective β1 and β2 blocker; No worries about peripheral vasospasms Aryloxypropanolamines; selective α-1 blocker; nonselective β1 and β2 blocker 9
