Question | Answer |
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 |