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Pharmacokinetics and Basic Pharmacology Concepts

A1 receptor (Gq) increases vascular smooth muscle contraction, of the skin, splanchnic nerves, GI tract and uterus muscle
A2 receptor (Gi) Decreases sympathetic outflow, decreases insulin release[inhibition and relaxation]
B1 receptor (Gs) Increases Heart Rate, aqueous humor formation, lipolysis, renin release, and contractility
B2 receptor (Gs) vasodilation, bronchodilation, and increases glucagon release, heart rate, contractility, lipolysis, relaxes uterine muscle
M1 receptor (Gq) CNS and enteric nervous system
M2 receptor (Gi) decreases heart rate and contractility
M3 receptor (Gq) Increase exocrine gland secretions, gut peristalsis, bladder contraction
D1 receptor (Gs) relaxes renal vascular smooth muscle
D2 receptor (Gi) moduates transmitter release esp in the brain
H1 receptor (Gq) increase in nasal and broncial mucous production, contraction of bronchioles, Pruritis and pain
H2 receptor (Gs) Increases gastric acid production
V1 receptor (Gq) Increases vascular smooth muscle contraction
V2 receptor (Gs) H20 Permeability and Reabsorption in the collecting tubules of the kidney
activation of Gq protiens Increase IP3 which increases intracellular Ca2+, and Increase in DAG which increases Protein Kinase C
activation of Gs proteins increase cAMP and protein kinase A
Activtion of Gi proteins decrease cAMP and protein kinase A
epinephrine (alpha agonist) increases outflow of aq. humor
Bromonodine (alpha agonist) decreases aq humor synthesis
Timolol, betaxolol, carteolol (B-blockers) decrease aq humor secretions
Azetozolamide (diuretics) decrease aq humor secretion due to HCO3- inhibition of carbonic anhydrase
Pilocarpine, Carbechol, Physostigmine, ecothiophate (Cholinomimetics) increase in aqueous humor, contract ciliary muscle to open trabecular meschwork.
Prostaglandin, Latanoprost Increase in aqueous humor and may darken the color of iris
Epinephrine A1,A2, B1, B2 low doses selective for B1 ; anaphylaxis, glaucoma (open angle), and asthma, hypotension
Norepinephrine A1 A2 >B1; hypotension but decrease in renal perfusion
Isoproternol B1=B2, AV BLOCK RARE
Dopamine D1=D2>B>a; shock (increase renal perfusion), heart failure
Dobutamine B1>B2; shock, heart failure, cardiac stress testing
Amphetamine Indirect agonist that releases stored catcecholamines; used for narcolepsy, ADD, and obesity
Ephedrine indirect agonist that releases stored catecholamines; used for nasal congestion, hypotension, urinary retention
Phenylephrine A1>A2; pupil dilator, vasoconstriction, and nasal decongestion
Albuterol, terbutaline B2>B1; asthma, COPD
Cocaine indirect general agonist, uptake inhibitor, causing vasoconstriction, and local anasthesia
Clonidine and a-methyldopa centrally acting alpah agonist, decreases adrnergic outflow, used for hypertension, esp with renal disease (no decrease in blood flow to the kidney)
antidote for acetominophine N-acetylcystein
antidote for salicylates alkalinize urine, dialysis
antidote for anticholinesterases (neostigmine, pyrdostigmine, edrophonium, PHysostigmine, Echothiophate), and Organophosphates Atropine +pralidoxime
antidote for antimuscarinic,antocholinergic agents PHysostigmine salicylate
B-blockers antidote glucagon
digitalis antitode Stop dig, normalize K+, lidocain, anti-dig Fab fragments, Mg2+
Iron antidote deferoxamine
LEad CaEDTA, dimercaprol, succimer, penicillamine
Arsenic, Mercury, gold Dimercaprol (BAL) succimer
Copper, arsenic, gold Penicillamine
Cyanaide Nitrite, B12
Methemoglobin methylene blue
carbon monoxide 100% O2 hyperbaric oxygen
Methanol, antifreeze ehtanol, dialysis, fomepizole
Opiods (morphine, fentanyl, heroine, codeine, methadone, meperidine, dextromethorpan) Naloxone/Naltroxone
Benzodiazepines (Diazepam, lorazepam, triazolam, temazepam, oxazepam..) Flumazenil competitive antagonist at GABA receptor
TCA (imipramine, amitriptyline, desipramine, nortiptyline, compiramine, doxepine) NaHCO3 (sodium bicarbonate)
Heparin protamin
warfarin vitamin K, fresh frozen plasma
tPA, streptokinase Amnocaproic acid
P450 Inducers Queen Barbra takes Phen phen Refuses Greasy CarbS: Quinidine, Barbituates, Phenytoin, Rifampin, Greosulvin, Carbamazepine, St. Johns Worts, Chronic EtOH
P450 Inhibitors Inhibitors Stop Cyber Kids from Eating Grapefruits: Sulfonamides, Cimetidine, Ketocanazole, Erythromycin (macrolide), Grapefruit Juice, verapamil, acute EtoH, disulfuram, steroids
Volume distribution equation (Vd) Vd = amount of drug in body/ plasma drug concentration
low Vd distribution in plasma
Medium Vd distrubiton in extracellular tissues
High Vd distrubition In tissues
Clearance (CL) CL= Rate of elimination of drug/ plasma drug concentration = Vd x Ke (elimination constant)
Half life t 1/2 T1/2 = .7 x Vd/ CL
Created by: Roshani



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