Pharmacokinetics and Basic Pharmacology Concepts
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| A1 receptor (Gq) | increases vascular smooth muscle contraction, of the skin, splanchnic nerves, GI tract and uterus muscle
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| A2 receptor (Gi) | Decreases sympathetic outflow, decreases insulin release[inhibition and relaxation]
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| B1 receptor (Gs) | Increases Heart Rate, aqueous humor formation, lipolysis, renin release, and contractility
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| B2 receptor (Gs) | vasodilation, bronchodilation, and increases glucagon release, heart rate, contractility, lipolysis, relaxes uterine muscle
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| M1 receptor (Gq) | CNS and enteric nervous system
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| M2 receptor (Gi) | decreases heart rate and contractility
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| M3 receptor (Gq) | Increase exocrine gland secretions, gut peristalsis, bladder contraction
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| D1 receptor (Gs) | relaxes renal vascular smooth muscle
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| D2 receptor (Gi) | moduates transmitter release esp in the brain
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| H1 receptor (Gq) | increase in nasal and broncial mucous production, contraction of bronchioles, Pruritis and pain
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| H2 receptor (Gs) | Increases gastric acid production
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| V1 receptor (Gq) | Increases vascular smooth muscle contraction
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| V2 receptor (Gs) | H20 Permeability and Reabsorption in the collecting tubules of the kidney
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| activation of Gq protiens | Increase IP3 which increases intracellular Ca2+, and Increase in DAG which increases Protein Kinase C
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| activation of Gs proteins | increase cAMP and protein kinase A
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| Activtion of Gi proteins | decrease cAMP and protein kinase A
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| epinephrine (alpha agonist) | increases outflow of aq. humor
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| Bromonodine (alpha agonist) | decreases aq humor synthesis
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| Timolol, betaxolol, carteolol (B-blockers) | decrease aq humor secretions
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| Azetozolamide (diuretics) | decrease aq humor secretion due to HCO3- inhibition of carbonic anhydrase
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| Pilocarpine, Carbechol, Physostigmine, ecothiophate (Cholinomimetics) | increase in aqueous humor, contract ciliary muscle to open trabecular meschwork.
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| Prostaglandin, Latanoprost | Increase in aqueous humor and may darken the color of iris
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| Epinephrine | A1,A2, B1, B2 low doses selective for B1 ; anaphylaxis, glaucoma (open angle), and asthma, hypotension
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| Norepinephrine | A1 A2 >B1; hypotension but decrease in renal perfusion
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| Isoproternol | B1=B2, AV BLOCK RARE
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| Dopamine | D1=D2>B>a; shock (increase renal perfusion), heart failure
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| Dobutamine | B1>B2; shock, heart failure, cardiac stress testing
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| Amphetamine | Indirect agonist that releases stored catcecholamines; used for narcolepsy, ADD, and obesity
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| Ephedrine | indirect agonist that releases stored catecholamines; used for nasal congestion, hypotension, urinary retention
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| Phenylephrine | A1>A2; pupil dilator, vasoconstriction, and nasal decongestion
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| Albuterol, terbutaline | B2>B1; asthma, COPD
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| Cocaine | indirect general agonist, uptake inhibitor, causing vasoconstriction, and local anasthesia
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| 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)
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| antidote for acetominophine | N-acetylcystein
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| antidote for salicylates | alkalinize urine, dialysis
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| antidote for anticholinesterases (neostigmine, pyrdostigmine, edrophonium, PHysostigmine, Echothiophate), and Organophosphates | Atropine +pralidoxime
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| antidote for antimuscarinic,antocholinergic agents | PHysostigmine salicylate
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| B-blockers antidote | glucagon
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| digitalis antitode | Stop dig, normalize K+, lidocain, anti-dig Fab fragments, Mg2+
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| Iron antidote | deferoxamine
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| LEad | CaEDTA, dimercaprol, succimer, penicillamine
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| Arsenic, Mercury, gold | Dimercaprol (BAL) succimer
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| Copper, arsenic, gold | Penicillamine
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| Cyanaide | Nitrite, B12
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| Methemoglobin | methylene blue
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| carbon monoxide | 100% O2 hyperbaric oxygen
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| Methanol, antifreeze | ehtanol, dialysis, fomepizole
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| Opiods (morphine, fentanyl, heroine, codeine, methadone, meperidine, dextromethorpan) | Naloxone/Naltroxone
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| Benzodiazepines (Diazepam, lorazepam, triazolam, temazepam, oxazepam..) | Flumazenil competitive antagonist at GABA receptor
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| TCA (imipramine, amitriptyline, desipramine, nortiptyline, compiramine, doxepine) | NaHCO3 (sodium bicarbonate)
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| Heparin | protamin
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| warfarin | vitamin K, fresh frozen plasma
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| tPA, streptokinase | Amnocaproic acid
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| P450 Inducers | Queen Barbra takes Phen phen Refuses Greasy CarbS: Quinidine, Barbituates, Phenytoin, Rifampin, Greosulvin, Carbamazepine, St. Johns Worts, Chronic EtOH
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| P450 Inhibitors | Inhibitors Stop Cyber Kids from Eating Grapefruits: Sulfonamides, Cimetidine, Ketocanazole, Erythromycin (macrolide), Grapefruit Juice, verapamil, acute EtoH, disulfuram, steroids
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| Volume distribution equation (Vd) | Vd = amount of drug in body/ plasma drug concentration
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| low Vd distribution | in plasma
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| Medium Vd distrubiton | in extracellular tissues
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| High Vd distrubition | In tissues
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| Clearance (CL) | CL= Rate of elimination of drug/ plasma drug concentration = Vd x Ke (elimination constant)
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| Half life t 1/2 | T1/2 = .7 x Vd/ CL
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Created by:
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