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395 Cards in this Set
- Front
- Back
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Question
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Answer
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28-year-old chemist presents with MPTP exposure. What neurotransmitter is depleted?
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Dopamine.
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Woman taking tetracycline exhibits photosensitivity.
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Rash on sun-exposed regions of the body.
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African-American man who goes to Africa develops a hemolytic anemia after taking malarial prophylaxis.
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Glucose-6-phosphate dehydrogenase deficiency
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Farmer presents with dyspnea, salivation, miosis, diarrhea, cramping, and blurry vision.
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Insecticide poisoning; inhibition of acetylcholinesterase.
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27-year-old female with a history of psychiatric illness now has urinary retention due to a neuroleptic. What do you treat it with?
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Bethanechol.
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Patient with recent kidney transplant is on cyclosporine for immunosuppression. Requires antifungal agent for candidiasis. What antifungal drug would result in cyclosporine toxicity?
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Ketoconazole.
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Patient is on carbamazepine. What routine workup should always be done?
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LFTs.
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23-year-old female who is on rifampin for TB prophylaxis and on birth control (estrogen) gets pregnant. Why?
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Rifampin augments estrogen metabolism in the liver, rendering it less effective.
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Km reflects
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the affinity of the enzyme for its substrate.
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Vmax is directly proportional
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to the enzyme concentration.
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The lower the Km, the
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The lower the Km, the higher the affinity.
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The ???? the Km, the higher the affinity.
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lower
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Competitive inhibitors vs Noncompetitive inhibitors WRT Resemble substrate
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Competitive-- Yes Noncompetitive-- NO
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Competitive inhibitors vs Noncompetitive inhibitors WRT Overcome by ↑ [S]
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Competitive-- Yes Noncompetitive-- NO
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Competitive inhibitors vs Noncompetitive inhibitors WRT Bind active site
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Competitive-- Yes Noncompetitive-- NO
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Competitive inhibitors vs Noncompetitive inhibitors WRT Effect on Vmax
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Competitive-- no change Noncompetitive-- decrease
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Competitive inhibitors vs Noncompetitive inhibitors WRT Effect on Km
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Competitive-- increase Noncompetitive-- no change
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Volume of distribution (Vd) describe and altered by
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Relates the amount of drug in the body to the plasma concentration. Vd of plasma protein–bound drugs can be altered by liver and kidney disease.
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Vd equation
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amount of drug in the body / plasma drug concentration
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Vd ranges and what the mean for where the drug is
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low Vd distribute in plasma medium Vd distribute in extracellular space high Vd distribute in tissues
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t1/2 =
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0.7 × Vd/CL
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0.7 × Vd/CL =
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half life
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concentration after # of half-lives
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1 - 50% 2 - 75% 3 - 87.5 3.3 - 90% 4 - 94%
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Loading dose =
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Cp × Vd/F.
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28 year old chemist presents with MPTP exposure What NT is depleted?
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Dopamine
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Woman taking tetracycline exhibits photosensitivity What are the clinical manifestations?
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Rash on sun-exposed regions of body
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Nondiabetic patient presents with hypoglycemia but low levels of C peptide What is the diagnosis
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Surreptitious insulin injection
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African American male who goes to Africa develops hemolytic anemia after taking malaria prophylaxis What is the enzyme defficiency
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Glucose 6 phosphate dehydrogenase
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27 year old female with history of psychiatric illness now has urinary retention due to neuroleptic What do you treat it with?
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Bethanechol
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Farmer presents with dyspnea, salivation, miosis, diarrhea, cramping and blurry vision What caused this and what is the mechanism
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Insecticide poisoning, inhibition of acetylcholinesterase
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Patient with recent kidney transplant is on cyclosporine for immunosuppresion, he requires antifungal agent for candidiasis What antifungal drug would result in cyclosporine toxicity?
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Ketoconazole
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Man on several medications including antidepressants and antihypertensives, has mydriasis and becomes constipated What is the cause of symptoms?
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TCA
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55 year old postmenopausal woman on tamoxifen therapy What is she at increased risk of acquiring?
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Endometrial carcinoma
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Woman on MAO inhibitor has hypertensive crisis after meal What did she ingest?
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Tyramine (wine or cheese)
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After taking clindamycin, patient develops toxic megacolon and diarrhea What is the mechanism of diarrhea?
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Clostridium difficile overgrowth
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Man starts a medication for hyperlipidemia. He then develops rash, pruritus and GI upset What drug was it?
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Niacin
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Patient is on carbamazepine What routine workup should be done?
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LFT's
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23 year old female who is on rifampin for TB prophylaxis and on birth control (estrogen) gets pregnant Why?
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Rifampin augments estrogen metabolism in liver rendering it less effective
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Patient develops cough and must discontinue captopril WHat is a good replacement drug and why doesnt it have the same side effects?
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Losartan - an angiotensin II receptor antagonist, does not increase bradykinin as captopril does
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Relates the amount of drug in the body to plasma concentration
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Vd - volume of distribution
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Formule for volume of distribution
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Vd = amount of drug in the body/plasma drug concentration
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Vd of plasma protein-bound drugs can be altered by what disease?
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Liver and kidney
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Relates the rate of elimination to plasma concentration
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CLEARANCE
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Formula for clearance
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Cl = rate of elimination of drug/plasma drug concentration
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The time required to change the amount of drug in the body by 1/2 during elimination (or during constant infusion) is called _
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Half life T1/2
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After 1 half life concentration of drug equals _ %
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50%
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After 2 half lifes concentration of drug equals_
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75%
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A drug infused at constant rate reaches about _ % of steady state after 4 T1/2
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94
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Formula for T1/2
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T1/2 = 0.7 * Vd/CL
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Loading dose formula
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Loading dose = Cp * Vd/F Cp= target plasma concentration F = bioavailibility
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Formula for maintenance dose
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Cp * CL / F Cp = target plasma concentration F = bioavailibility
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In patients with impaired renal or hepatic function, the loading dose decreases, increases or remains unchanged? Maintenance dose?
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Loading dose remains unchanged Maintenance dose decreases
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Rate of elimination is constant (constant amount of drug is eliminated per unit time) - what order elimination? What happens to target plasma concentration?
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Zero order elimination Target plasma concentration decreases linearly with time
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Rate of elimination is proportional to drug concentration (constant fraction of drug eliminated per unit time) - what order elimination? What happens to target plasma concentration?
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First order elimination Cp decreases exponentially with time
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Give examples of drugs with zero order elimination
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Ethanol Phenytoin Aspirin (at high or toxic concentration)
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Phase I metabolism products, what happens and how eliminated
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(reduction, oxidation, hydrolysis) yields _ slightly polar, water-soluble metabolites (often still active) not yet eliminated
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What phase of metabolism associated with cytochrome P450
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Phase I
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What phase of metabolism associated with conjugation
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Phase II
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Phase II metabolism products, what happens and how eliminated
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acetylation, glucoronidation, sulfation) yields Very polar, inactive metanolites (renally excreted)
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Geriatric patients lose which phase of metabolism first?
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Phase I
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Is it safe? Pharmacokinetics? - which phase of clinical testing of the drug
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Phase I
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Does it work in patients?- which phase of clinical testing of the drug
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Phase II
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Does it work? Double blind - which phase of clinical testing of the drug
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Phase III
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What happens in phase IV of clinical testing of the drug
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Postmarketing surveillance
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A competitive antagonist shifts agonist curve where?
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To the right
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A noncompetitive antagonist (irreversible) shifts agonist curve where?
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Downward
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Urine pH and drug elimination what is trapped
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Ionized species get trapped.
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Urine pH and drug elimination Ionized species
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Ionized species get trapped.
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Urine pH and drug elimination Weak acids what and Tx
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Trapped in basic environments. Treat overdose with bicarbonate.
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Urine pH and drug elimination Weak bases what and Tx
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Trapped in acidic environments. Treat overdose with ammonium chloride.
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Urine pH and drug elimination Trapped in basic environments.
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Weak acids
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Urine pH and drug elimination Trapped in acidic environments.
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Weak bases
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dose response curves and different antagonists
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A. A competitive antagonist shifts curve to the right, decreasing potency and ↑ EC50. B. A noncompetitive antago- nist shifts the agonist curve downward, decreasing efficacy.
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dose response curves and shifts curve to the right, decreasing potency and ↑ EC50.
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competitive antagonist
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dose response curves and shifts the curve downward, decreasing efficacy.
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noncompetitive antago- nist
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dose response curves and in a system with spare receptors
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the EC50 is lower than the Kd, indicating that to achieve 50% of maximum effect, < 50% of the receptors must be activated. EC50: dose causing 50% of maximal effect. Kd: concentration ofdrug required to bind 50% of receptor sites.
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dose response curves and different agonists
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1. The partial agonist acts on the same receptor system as the full agonist but has a lower maximal efficacy no matter the dose. A partial agonist may be more potent (as in the figure), less potent, or equally potent; potency is an independent factor.
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dose response curves and may be more potent (as in the figure), less potent, or equally potent; potency is an independent factor.
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A partial agonist
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Efficacy
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#NAME?
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Potency
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#NAME?
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#NAME?
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Potency
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#NAME?
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Efficacy
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Therapeutic index
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TILE LD50/ED50
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pre and postsynaptic nervous system neurotransmitters Parasymp
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ACh (nicotinic) ACh (muscarinic)
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pre and postsynaptic nervous system neurotransmitters Somatic
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only one ACh (nicotinic)
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pre and postsynaptic nervous system neurotransmitters Sympathetic
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pre = ACh (nicotinic) Ach (muscarinic)- sweat glands NEα,β - Cardiac and smooth muscle, gland cells, nerve terminals D1 - Renal vascular smooth muscle
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nicotinic receptor mech
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ACh ligand gated Na+/K+ channels
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muscarinic receptor mech
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ACh G- protein coupled receptors that act through 2nd messengers
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ACh ligand gated Na+/K+ channels
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nicotinic receptor
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ACh G- protein coupled receptors that act through 2nd messengers
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muscarinic receptor
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G-protein-linked 2nd messengers give G protein and major function α1 Receptor
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q ↑ vascular smooth muscle contraction
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G-protein-linked 2nd messengers give G protein and major function α2 Receptor
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i ↓ sympathetic outflow, ↓ insulin release
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G-protein-linked 2nd messengers give G protein and major function β1 Receptor
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s ↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous humor formation
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G-protein-linked 2nd messengers give G protein and major function β2 Receptor
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s Vasodilation, bronchodilation, ↑ glucagon release
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G-protein-linked 2nd messengers give G protein and major function M1 Receptor
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q CNS
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G-protein-linked 2nd messengers give G protein and major function M2 Receptor
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i ↓ heart rate
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G-protein-linked 2nd messengers give G protein and major function M3 Receptor
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q ↑ exocrine gland secretions
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G-protein-linked 2nd messengers give G protein and major function D2 Receptor
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i Modulates transmitter release, especially in brain
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G-protein-linked 2nd messengers give G protein and major function D1 Receptor
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s Relaxes renal vascular smooth muscle
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G-protein-linked 2nd messengers give G protein and major function H1 Receptor
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q ↑ nasal and bronchial mucus production, contraction of bronchioles,pruritus, and pain
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G-protein-linked 2nd messengers give G protein and major function H2 Receptor
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s ↑ gastric acid secretion
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G-protein-linked 2nd messengers give G protein and major function V1 Receptor
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q ↑ vascular smooth muscle contraction
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G-protein-linked 2nd messengers give G protein and major function V2 Receptor
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s ↑ H2O permeability and reabsorption in the collecting tubules of the kidney
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Given the major function and G-protein class name the receptor q ↑ vascular smooth muscle contraction
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α1
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Given the major function and G-protein class name the receptor i ↓ sympathetic outflow, ↓ insulin release
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α2
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Given the major function and G-protein class name the receptor s ↑ heart rate, ↑ contractility, ↑ renin release, ↑ lipolysis, ↑ aqueous humor formation
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β1
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Given the major function and G-protein class name the receptor s Vasodilation, bronchodilation, ↑ glucagon release
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β2
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Given the major function and G-protein class name the receptor q CNS
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M1
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Given the major function and G-protein class name the receptor i ↓ heart rate
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M2
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Given the major function and G-protein class name the receptor q ↑ exocrine gland secretions
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M3
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Given the major function and G-protein class name the receptor s Relaxes renal vascular smooth muscle
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D1
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Given the major function and G-protein class name the receptor i Modulates transmitter release, especially in brain
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D2
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Given the major function and G-protein class name the receptor q ↑ nasal and bronchial mucus production, contraction of bronchioles,
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H1
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Given the major function and G-protein class name the receptor s ↑ gastric acid secretion
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H2
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Given the major function and G-protein class name the receptor q ↑ vascular smooth muscle contraction
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V1
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Given the major function and G-protein class name the receptor s ↑ H2O permeability and reabsorption in the collecting tubules of the kidney
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V2
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G-protein-linked 2nd messengers Receptor G-protein class how to remember which goes with which
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α1, α2, β1, β2, M1, M2, M3, D1, D2, H1, H2, V1, V2 "QISS (kiss) and QIQ (kick) till you're SIQ (sick) of SQS (sex)."
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G-protein-linked 2nd messengers Receptor G-protein class 3rd messengers... for Gq
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HAVe 1 M&M (H1, α1, V1, M1, M3) ↑ Phospholipase C to IP3 (↑Ca2+) and DAG (Protein Kinase C)
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G-protein-linked 2nd messengers Receptor G-protein class 3rd messengers... for Gs
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β1, β2, D1 H2, V2 ↑ Adenylcyclase (↑ATP to cAMP [ ↑ Protein kinase A])
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G-protein-linked 2nd messengers Receptor G-protein class 3rd messengers for... Gi
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MAD 2's (M2, α2, D2) ↓Adenylcyclase (↓ATP to cAMP [ ↑ Protein kinase A])
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Release of NE from a sympathetic nerve ending is modulated by with mech
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by NE itself, acting on presynaptic α2 autoreceptors, and by ACh, angiotensin II, and other substances.
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Cholinomimetics direct names
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Bethanechol Carbachol Pilocarpine Methacholine
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Cholinomimetics indirect names
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Neostigmine Pyridostigmine Edrophonium Physostigmine Echothiophate
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Bethanechol Mech
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Cholinomimetics: Direct agonist
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Carbachol Mech
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Cholinomimetics: Direct agonist
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Pilocarpine Mech
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Cholinomimetics: Direct agonist
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Methacholine Mech
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Cholinomimetics: Direct agonist
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Neostigmine Mech
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Cholinomimetics: inirect agonist (anticholinesterase) ↑ endogenous ACh
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Pyridostigmine Mech
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Cholinomimetics: inirect agonist (anticholinesterase) ↑ endogenous ACh
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Edrophonium Mech
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Cholinomimetics: inirect agonist (anticholinesterase) ↑ endogenous ACh
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Physostigmine Mech
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Cholinomimetics: inirect agonist (anticholinesterase) ↑ endogenous ACh
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Echothiophate Mech
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Cholinomimetics: inirect agonist (anticholinesterase) ↑ endogenous ACh
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Which Cholinergic Activates Bowel and Bladder smooth muscle;
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Bethanechol
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Which Cholinergic Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle)
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Carbachol
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Which Cholinergic Stimulates muscarinic receptors in airway when inhaled.
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Methacholine
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Which Cholinergic Potent stimulator of sweat, tears, saliva
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Pilocarpine
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Which Cholinergic resistant to AChE
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Bethanechol and Pilocarpine
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Which Cholinergic ↑ endogenous ACh No CNS penetration
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Neostigmine
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Which Cholinergic ↑ endogenous ACh; ↑ strength
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Pyridostigmine
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Which Cholinergic is used for Postoperative and neurogenic ileus and urinary retention
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Bethanechol and Neostigmine
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Which Cholinergic is used for Glaucoma, pupillary contraction, and release of intraocular pressure
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Carbachol, Echothiophate and Physostigmine
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Which Cholinergic is used for Potent stimulator of sweat, tears, saliva
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Pilocarpine
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Which Cholinergic is used for Challenge test for diagnosis of asthma
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Methacholine
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Which Cholinergic is used for reversal of neuromuscular junction blockade (postoperative)
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Neostigmine
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Which Cholinergic is used for Myasthenia gravis
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Neostigmine Pyridostigmine does penetrate CNS
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Which Cholinergic is used for Diagnosis of myasthenia gravis
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Edrophonium
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Which Cholinergic is used for atropine overdose
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Physostigmine
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Clinical applications of Bethanechol
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Postoperative and neurogenic ileus and urinary retention
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Clinical applications of Carbachol
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Glaucoma, pupillary contraction, and release of intraocular pressure
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Clinical applications of Pilocarpine
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Potent stimulator of sweat, tears, saliva
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Clinical applications of Methacholine
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Challenge test for diagnosis of asthma
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Clinical applications of Neostigmine
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Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative)
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Clinical applications of Pyridostigmine
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Myasthenia gravis; does penetrate CNS
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Clinical applications of Edrophonium
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Diagnosis of myasthenia gravis (extremely short acting)
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Clinical applications of Physostigmine
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Glaucoma (crosses blood-brain barrier → CNS) and atropine overdose
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Clinical applications of Echothiophate
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Glaucoma
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which anticholinesterase is extremely short acting
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Edrophonium
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Cholinesterase inhibitor poisoning symps
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DUMBBEL ASS. Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Abdominal cramping, Sweating, and Salivation
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Cholinesterase inhibitor poisoning Tx
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Atropine (muscarinic antagonist) plus pralidoxime
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chemical antagonist used to regenerate active cholinesterase
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pralidoxime
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pralidoxime uses and mech
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Cholinesterase inhibitor poisoning chemical antagonist used to regenerate active cholinesterase
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Parathion
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organophosphate
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organophosphate toxicity mech
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Irreversible Cholinesterase inhibitor poisoning
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Atropine, mech
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Muscarinic antagonist
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Benztropine mech
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Muscarinic antagonist
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Scopolamine mech
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Muscarinic antagonist
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Ipratropium mech
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Muscarinic antagonist
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Methscopolamine, oxybutin, glycopyrrolate mech
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Muscarinic antagonist
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Atropine clinical use
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Produce mydriasis and cycloplegia
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Benztropine clinical use
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Parkinson’s disease
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Scopolamine clinical use
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Motion sickness
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Ipratropium clinical use
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Asthma, COPD
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Methscopolamine, oxybutin, glycopyrrolate clinical use
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Reduce urgency in mild cystitis and reduce bladder spasms
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Glaucoma drugs mech and side effects Epinephrine
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↑ outflow of aqueous humor Mydriasis, stinging; do not use in closed-angle glaucoma
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Glaucoma drugs mech and side effects Brimonidine
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↓ aqueous humor synthesis No pupillary or vision changes
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Glaucoma drugs mech and side effects β-blockers
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↓ aqueous humor secretion No pupillary or vision changes
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Glaucoma drugs mech and side effects Acetazolamide
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↓ aqueous humor secretion due to ↓ HCO3− (via inhibition of carbonic anhydrase) No pupillary or vision changes
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Glaucoma drugs mech and side effects Cholinomimetics
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↑ outflow of aqueous humor; contract ciliary muscle and open trabecular meshwork; Miosis, cyclospasm
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Glaucoma drugs mech and side effects Latanoprost (PGF2α)
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↑ outflow of aqueous humor Darkens color of iris (browning)
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which glaucoma drug ↑ outflow of aqueous humor
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Epinephrine Cholinomimetics Prostaglandin (Latanoprost (PGF2α))
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which glaucoma drug ↓ aqueous humor synthesis
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Brimonidine
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which glaucoma drug ↓ aqueous humor secretion
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β-blockers: Timolol, betaxolol, carteolol Diuretics: Acetazolamide
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which glaucoma drug causes Mydriasis, stinging; do not use in closed-angle glaucoma
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Epinephrine
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which glaucoma drug causes Miosis, cyclospasm
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Cholinomimetics
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which glaucoma drug causes Darkens color of iris (browning)
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Prostaglandin: Latanoprost (PGF2α)
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Atropine effects
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dilates pupils and Blocks SLUD: ↓Salivation ↓Lacrimation ↓Urination ↓Defecation
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Atropine Toxicity
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Hot as a hare Dry as a bone Red as a beet Blind as a bat Mad as a hatter
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Can cause acute angle-closure glaucoma in elderly, urinary retention in men with prostatic hypertrophy, and hyperthermia in infants.
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Atropine
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Hexamethonium Mechanism
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Nicotinic ACh receptor antagonist. Ganglionic blocker.
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Hexamethonium Clinical use
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Ganglionic blocker. Used in experimental models to prevent vagal reflex responses to changes in blood pressure– –e.g., prevents reflex bradycardia caused by NE.
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prevents reflex bradycardia caused by NE
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Hexamethonium
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Used in experimental models to prevent vagal reflex responses to changes in blood pressure
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Hexamethonium
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selectivity for Sympathomimetics Epinephrine
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α1, α2, β1, β2, low doses selective for β1
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selectivity for Sympathomimetics NE
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α1, α2 >β1
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selectivity for Sympathomimetics Isoproterenol
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β1 =β2
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selectivity for Sympathomimetics Dopamine
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D1 = D2 >β >α
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selectivity for Sympathomimetics Dobutamine
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β1 >β2
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Mechanism for Sympathomimetics Amphetamine
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Indirect general agonist, releases stored catecholamines
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Mechanism for Sympathomimetics Ephedrine
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Indirect general agonist, releases stored catecholamines
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Mechanism forSympathomimetics Cocaine
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Indirect general agonist, uptake inhibitor
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Mechanism for Sympathomimetics Clonidine, α-methyldopa
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Centrally acting α-agonist, ↓ central adrenergic outflow
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selectivity for Sympathomimetics Phenylephrine
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α1 >α2
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selectivity for Sympathomimetics Albuterol
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β2 >β1
|
|
|
Mechanism/selectivity for Sympathomimetics terbutaline
|
β2 >β1
|
|
|
name the Sympathomimetic α1, α2, β1, β2, low doses selective for β1
|
Epinephrine
|
|
|
name the Sympathomimetic α1, α2 >β1
|
NE
|
|
|
name the Sympathomimetic β1 =β2
|
Isoproterenol
|
|
|
name the Sympathomimetic β1 >β2
|
Dobutamine
|
|
|
name the Sympathomimetic D1 = D2 >β >α
|
Dopamine
|
|
|
name the Sympathomimetic Indirect general agonist, releases stored catecholamines
|
Amphetamine and Ephedrine
|
|
|
name the Sympathomimetic α1 >α2
|
Phenylephrine
|
|
|
name the Sympathomimetic β2 >β1
|
Albuterol, terbutaline
|
|
|
name the Sympathomimetic Indirect general agonist, uptake inhibitor
|
Cocaine
|
|
|
name the Sympathomimetic Centrally acting α-agonist, ↓ central adrenergic outflow
|
Clonidine, α-methyldopa
|
|
|
effect on BP and HR of Norepinephrine
|
(α > β) ↑ BP ↓ HR (reflex bradycardia)
|
|
|
effect on BP and HR of Epinephrine
|
nonselective NC BP( increases systolic, but decreases diastolic)
|
|
|
effect on BP and HR of Isoproterenol
|
(β > α) ↓ BP ↑ HR
|
|
|
Applications of Sympathomimetics Epinephrine
|
Anaphylaxis, glaucoma (open angle), asthma, hypotension
|
|
|
Applications of Sympathomimetics NE
|
Hypotension (but ↓ renal perfusion)
|
|
|
Applications of Sympathomimetics Isoproterenol
|
AV block (rare)
|
|
|
Applications of Sympathomimetics Dopamine
|
Shock (↑ renal perfusion), heart failure
|
|
|
Applications of Sympathomimetics Dobutamine
|
Shock, heart failure cardiac stress testing
|
|
|
Applications of Sympathomimetics Amphetamine
|
Narcolepsy, obesity, ADHD
|
|
|
Applications of Sympathomimetics Ephedrine
|
Nasal decongestion, urinary incontinence, hypotension
|
|
|
Applications of Sympathomimetics Phenylephrine
|
Pupil dilator, vasoconstriction, nasal decongestion
|
|
|
Applications of Sympathomimetics Albuterol, terbutaline
|
Asthma
|
|
|
Applications of Sympathomimetics Cocaine
|
Causes vasoconstriction and local anesthesia
|
|
|
Applications of Sympathomimetics Clonidine, α-methyldopa
|
Hypertension, especially with renal disease (no ↓ in blood flow to kidney)
|
|
|
name the Nonselective α-blockers
|
Phenoxybenzamine phentolamine
|
|
|
name the α1 selective α-blockers
|
Prazosin, terazosin, doxazosin
|
|
|
name the α2 selective α-blockers
|
Mirtazapine
|
|
|
Nonselective α-blockers Application and Toxicity
|
-Pheochromocytoma -Orthostatic hypotension, reflex tachycardia
|
|
|
α1 selective α-blockers Application and Toxicity
|
-Hypertension, urinary retention in BPH -1st-dose orthostatic hypotension, dizziness, headache
|
|
|
α2 selective α-blockers Application and Toxicity
|
-Depression -Sedation, ↑ serum cholesterol, ↑ appetite
|
|
|
Nonselective α-blockers names and differences
|
Phenoxybenzamine (irreversible) phentolamine (reversible)
|
|
|
effects of an α-blocker (e.g., phentolamine) on BP responses to epinephrine and phenylephrine.
|
The epinephrine response exhibits reversal of the mean blood pressure change, from a net increase (the α response) to a net decrease (the β2 response). The response to phenylephrine is suppressed but not reversed because phenylephrine is a “pure” α-agonist without β action.
|
|
|
β-blockers non selective ones
|
Nonselective (N or later)(β1 = β2)––propranolol, timolol, nadolol, pindolol (partial agonist), and labetalol (partial agonist, and exception to the after N rule and the olol rule)
|
|
|
β-blockers selective ones
|
Before N β1 selective (β1 > β2)–– Betaxolol, Esmolol (short acting), Atenolol, Metoprolol Acebutolol (partial agonist hes and Ass),
|
|
|
β-blocker effect WRT Hypertension
|
↓ cardiac output, ↓ renin secretion
|
|
|
β-blocker effect WRT Angina pectoris
|
↓ heart rate and contractility, resulting in ↓ O2 consumption
|
|
|
β-blocker effect WRT MI
|
β-blockers ↓ mortality
|
|
|
β-blocker effect WRT SVT
|
↓ AV conduction velocity
|
|
|
β-blocker effect WRT CHF
|
Slows progression of chronic failure
|
|
|
β-blocker effect WRT Glaucoma
|
↓ secretion of aqueous humor
|
|
|
which β-blockers Tx for Glaucoma
|
timolol
|
|
|
which β-blockers Tx for SVT
|
propranolol, esmolol
|
|
|
β-blockers Toxicity (non cardiac)
|
1. Impotence, 2. exacerbation of asthma, 3. CNS adverse effects (sedation, sleep alterations); 4. diabetics can't feel low sugar
|
|
|
β-blockers Toxicity (cardiac)
|
-bradycardia, -AV block, -CHF
|
|
|
antidote for Acetaminophen
|
1. N-acetylcysteine
|
|
|
antidote for Salicylates
|
2. Alkalinize urine, dialysis
|
|
|
antidote for Anticholinesterases, organophosphates
|
3. Atropine, pralidoxime
|
|
|
antidote for Antimuscarinic, anticholinergic agents
|
4. Physostigmine salicylate
|
|
|
antidote for β-blockers
|
5. Glucagon
|
|
|
antidote for Digitalis
|
6. Stop dig, normalize K+, lidocaine, anti-dig Fab fragments, Mg2+
|
|
|
antidote for Iron
|
7. Deferoxamine
|
|
|
antidote for Lead
|
8. CaEDTA, dimercaprol, succimer, penicillamine
|
|
|
antidote for Arsenic, mercury, gold
|
9. Dimercaprol (BAL), succimer
|
|
|
antidote for Copper, arsenic, gold
|
10. Penicillamine
|
|
|
antidote for Cyanide
|
11. Nitrite, hydroxocobalamin, thiosulfate
|
|
|
antidote for Methemoglobin
|
12. Methylene blue
|
|
|
antidote for Carbon monoxide
|
13. 100% O , hyperbaric O
|
|
|
antidote for Methanol, ethylene glycol (antifreeze)
|
14. Ethanol, dialysis, fomepizole
|
|
|
antidote for Opioids
|
15. Naloxone/naltrexone
|
|
|
antidote for Benzodiazepines
|
16. Flumazenil
|
|
|
antidote for TCAs
|
17. NaHCO3 (nonspecific)
|
|
|
antidote for Heparin
|
18. Protamine
|
|
|
antidote for Warfarin
|
19. Vitamin K, fresh frozen plasma
|
|
|
antidote for tPA, streptokinase
|
20. Aminocaproic acid
|
|
|
antidote for Basic amphetamines
|
NH4CL (acidify urine)
|
|
|
This antidote is used for NH4CL (acidify urine)
|
Basic amphetamines
|
|
|
This antidote is used for Aminocaproic acid
|
tPA, streptokinase
|
|
|
This antidote is used for Vitamin K, fresh frozen plasma
|
Warfarin
|
|
|
This antidote is used for Protamine
|
Heparin
|
|
|
This antidote is used for NaHCO3 (nonspecific)
|
TCAs
|
|
|
This antidote is used for Flumazenil
|
Benzodiazepines
|
|
|
This antidote is used for N-acetylcysteine
|
1. Acetaminophen
|
|
|
This antidote is used for Alkalinize urine, dialysis
|
2. Salicylates
|
|
|
This antidote is used for Atropine, pralidoxime
|
3. Anticholinesterases, organophosphates
|
|
|
This antidote is used for Physostigmine salicylate
|
4. Antimuscarinic, anticholinergic agents
|
|
|
This antidote is used for Glucagon
|
5. β-blockers
|
|
|
This antidote is used for Stop dig, normalize K+, lidocaine, anti-dig Fab fragments, Mg2+
|
6. Digitalis
|
|
|
This antidote is used for Deferoxamine
|
7. Iron
|
|
|
This antidote is used for CaEDTA, dimercaprol, uccimer, penicillamine
|
8. Lead
|
|
|
This antidote is used for Dimercaprol (BAL), succimer
|
9. Arsenic, mercury, gold
|
|
|
This antidote is used for Penicillamine
|
10. Copper, arsenic, gold
|
|
|
This antidote is used for Nitrite, hydroxocobalamin, thiosulfate
|
11. Cyanide
|
|
|
This antidote is used for Methylene blue
|
12. Methemoglobin
|
|
|
This antidote is used for 100% O2, hyperbaric O2
|
13. Carbon monoxide
|
|
|
This antidote is used for Ethanol, dialysis, fomepizole
|
14. Methanol, ethylene glycol (antifreeze)
|
|
|
This antidote is used for Naloxone/naltrexone
|
15. Opioids
|
|
|
signs of Lead poisoning
|
LEAD. -Lead Lines on gingivae and on epiphyses on x-ray. -Encephalopathy and RBC basophilic stippling. -Abdominal colic and sideroblastic Anemia. -Drops––wrist and foot drop.
|
|
|
Drug reaction by system Cardiovascular Atropine-like side effects
|
-Tricyclics
|
|
|
Drug reaction by system Cardiac toxicity
|
-Doxorubicin (Adriamycin), -daunorubicin
|
|
|
Drug reaction by system Coronary vasospasm
|
Cocaine
|
|
|
Drug reaction by system Cutaneous flushing
|
-Niacin, -Ca2+ channel blockers, -adenosine, -vancomycin
|
|
|
Drug reaction by system Torsades des pointes
|
-Class III (sotalol), -class IA (quinidine) -cisapride
|
|
|
Drug reaction by system Agranulocytosis
|
-Clozapine, -carbamazepine, -colchicine
|
|
|
Drug reaction by system Aplastic anemi
|
-Chloramphenicol, -benzene, -NSAIDs
|
|
|
Drug reaction by system Gray baby syndrome
|
Chloramphenicol
|
|
|
Drug reaction by system Hemolysis in G6PD- deficient patients
|
IS PAIN isoniazid (INH), Sulfonamides, primaquine, aspirin, ibuprofen, nitrofurantoin
|
|
|
Drug reaction by system Thrombotic complications
|
OCPs (e.g., estrogens and progestins)
|
|
|
Drug reaction by system Cough
|
ACE inhibitors
|
|
|
Drug reaction by system Pulmonary fibrosis
|
Bleomycin, amiodarone, busulfan
|
|
|
Drug reaction by system Acute cholestatic hepatitis
|
Macrolides
|
|
|
Drug reaction by system Focal to massive hepatic necrosis
|
Halothane, valproic acid, acetaminophen, Amanita phalloides
|
|
|
Drug reaction by system Hepatitis
|
INH
|
|
|
Drug reaction by system Pseudomembranous colitis
|
Clindamycin, ampicillin
|
|
|
Drug reaction by system Gynecomastia
|
(Some Drugs Create Awesome, Excellent Knockers) Spironolactone, Digitalis, Cimetidine, Alcohol chronicuse, Estrogens, Ketoconazole
|
|
|
Drug reaction by system Hot flashes
|
Tamoxifen
|
|
|
Drug reaction by system Gingival hyperplasia
|
Phenytoin
|
|
|
Drug reaction by system Osteoporosis
|
Corticosteroids, heparin
|
|
|
Drug reaction by system Photosensitivity
|
(SAT for a photo) Sulfonamides, Amiodarone, Tetracycline
|
|
|
Drug reaction by system SLE-like syndrome
|
(it’s not HIPP to have lupus)
|
|
|
Drug reaction by system Tendonitis, tendon rupture, and cartilage damage (kids)
|
Fluoroquinolones
|
|
|
Drug reaction by system Fanconi’s syndrome
|
Expired tetracycline
|
|
|
Drug reaction by system Interstitial nephritis
|
Methicillin
|
|
|
Drug reaction by system Hemorrhagic cystitis
|
Cyclophosphamide, ifosfamide
|
|
|
Drug reaction by system Cinchonism
|
Quinidine, quinine
|
|
|
Drug reaction by system Diabetes insipidus
|
Lithium, demeclocycline
|
|
|
Drug reaction by system Tardive dyskinesia
|
Antipsychotics
|
|
|
Drug reaction by system Disulfiram-like reaction
|
Metronidazole, certain cephalosporins, procarbazine, sulfonylureas
|
|
|
Drug reaction by system Nephrotoxicity/ neurotoxicity
|
Polymyxins
|
|
|
Drug reaction by system Nephrotoxicity/ ototoxicity
|
Aminoglycosides, loop diuretics, cisplatin
|
|
|
P-450 Inducers
|
"Queen Barb takes Phen-phen and Refuses Greasy Carved Steak" Quinidine (can inhibit too), Barbiturates, Phenytoin, Rifampin, Griseofulvin, Carbamazepine, St. John’s wort
|
|
|
P-450 Inhibitors
|
Inhibitors Stop Cyber-Kids from Eating Grapefruit. Isoniazid Sulfonamides Cimetidine Ketoconazole Erythromycin Grapefruit juice
|
|
|
Iron Poisioning Mech
|
Cell death due to peroxidation of membrane lipids
|
|
|
Iron Poisioning Symps
|
acute - gastric bleeding chronic - metabolic acidosis, scarring (leading to GI obstruction)
|
|
|
INHIBITED BY DISULFIRAM
|
Acetaldehyde dehydrogenase
|
|
|
COMPETITIVE SUBSTRATES FOR Alcohol dehydrogenase
|
-Ethylene glycol -Methanol -Ethanol
|
|
|
Alcohol toxicity Ethylene glycol
|
Acidosis, nephrotoxicity
|
|
|
Alcohol toxicity Methanol
|
Severe acidosis, retinal damage
|
|
|
Alcohol toxicity Ethanol
|
Nausea, vomiting, headache, hypotension
|
|
|
which Alcohol toxicity Acidosis, nephrotoxicity
|
Ethylene glycol
|
|
|
which Alcohol toxicity Severe acidosis, retinal damage
|
Methanol
|
|
|
which Alcohol toxicity Nausea, vomiting, headache, hypotension
|
Ethanol
|
|
|
Alcohol toxicity what causes the problem in Ethylene glycol
|
Build up of Oxalic acid
|
|
|
Alcohol toxicity what causes the problem in Methanol
|
Build up of Formaldehyde and formic acid
|
|
|
Alcohol toxicity what causes the problem in Ethanol
|
Build up of Acetaldehyde
|
|
|
which Alcohol toxicity Oxalic acid is the problem
|
Ethylene glycol
|
|
|
which Alcohol toxicity Formaldehyde and formic acid is the problem
|
Methanol
|
|
|
which Alcohol toxicity Acetaldehyde is the problem
|
Ethanol
|
|
|
Drugs that cause problems in patients with sulfa allergies
|
Celecoxib, furosemide, thiazides, TMP-SMX, sulfonyureas, sufasalazine
|
|
|
Herbal agents Clinical uses and Toxicities Echinacea
|
Common cold no major
|
|
|
Herbal agents Clinical uses and Toxicities Ephedra
|
As for ephedrine CNS and cardiovascular stimulation; arrhythmias, stroke, and seizures at high doses
|
|
|
Herbal agents Clinical uses and Toxicities Feverfew
|
Migraine mouth ulcers, antiplatelet actions
|
|
|
Herbal agents Clinical uses and Toxicities Ginkgo
|
Intermittent claudication anxiety, insomnia, antiplatelet actions
|
|
|
Herbal agents Clinical uses and Toxicities Kava
|
Chronic anxiety sedation, ataxia, hepatotoxicity, phototoxicity, dermatotoxicity
|
|
|
Herbal agents Clinical uses and Toxicities Milk thistle
|
Viral hepatitis Loose stools
|
|
|
Herbal agents Clinical uses and Toxicities Saw palmetto
|
Benign prostatic hyperplasia ↓ libido, hypertension
|
|
|
Herbal agents Clinical uses and Toxicities St. John’s wort
|
Mild to moderate depression phototoxicity; serotonin syndrome with SSRIs; induces P-450 system
|
|
|
Herbal agents Clinical uses and Toxicities Dehydroepiandrosterone
|
Symptomatic improvement in females with SLE or AIDS Androgenization (premenopausal women), estrogenic effects (postmenopausal), feminization (young men)
|
|
|
Herbal agents Clinical uses and Toxicities Melatonin
|
Jet lag, Sedation, suppresses midcycle LH, hypoprolactinemia
|
|
|
Drug name Ending / Category -afil
|
Erectile dysfunction
|
|
|
Drug name Ending / Category Erectile dysfunction
|
-afil
|
|
|
Drug name Ending / Category -ane
|
Inhalational general anesthetic
|
|
|
Drug name Ending / Category Inhalational general anesthetic
|
-ane
|
|
|
Drug name Ending / Category -azepam
|
Benzodiazepine
|
|
|
Drug name Ending / Category Benzodiazepine
|
-azepam
|
|
|
Drug name Ending / Category -azine
|
Phenothiazine (neuroleptic, antiemetic)
|
|
|
Drug name Ending / Category Phenothiazine (neuroleptic, antiemetic)
|
-azine
|
|
|
Drug name Ending / Category -azole
|
Antifungal
|
|
|
Drug name Ending / Category Antifungal
|
-azole
|
|
|
Drug name Ending / Category -barbital
|
Barbiturate
|
|
|
Drug name Ending / Category Barbiturate
|
-barbital
|
|
|
Drug name Ending / Category -caine
|
Local anesthetic
|
|
|
Drug name Ending / Category Local anesthetic
|
-caine
|
|
|
Drug name Ending / Category -cillin
|
Penicillin
|
|
|
Drug name Ending / Category Penicillin
|
-cillin
|
|
|
Drug name Ending / Category -cycline
|
Antibiotic, protein synthesis inhibitor
|
|
|
Drug name Ending / Category Antibiotic, protein synthesis inhibitor
|
-cycline
|
|
|
Drug name Ending / Category -ipramine
|
TCA
|
|
|
gjkgjh
|
ghjkghjkgh
|
|
|
Drug name Ending / Category Protease inhibitor
|
-navir
|
|
|
Drug name Ending / Category -navir
|
Protease inhibitor
|
|
|
Drug name Ending / Category -olol
|
β-antagonist
|
|
|
Drug name Ending / Category β-antagonist
|
-olol
|
|
|
Drug name Ending / Category -operidol
|
Butyrophenone (neuroleptic)
|
|
|
Drug name Ending / Category Butyrophenone (neuroleptic)
|
-operidol
|
|
|
Drug name Ending / Category -oxin
|
Cardiac glycoside (inotropic agent)
|
|
|
Drug name Ending / Category Cardiac glycoside (inotropic agent)
|
-oxin
|
|
|
Drug name Ending / Category -phylline
|
Methylxanthine
|
|
|
Drug name Ending / Category Methylxanthine
|
-phylline
|
|
|
Drug name Ending / Category -pril
|
ACE inhibitor
|
|
|
Drug name Ending / Category ACE inhibitor
|
-pril
|
|
|
Drug name Ending / Category -terol
|
β2 agonist
|
|
|
Drug name Ending / Category β2 agonist
|
-terol
|
|
|
Drug name Ending / Category -tidine
|
H2 antagonist
|
|
|
Drug name Ending / Category H2 antagonist
|
-tidine
|
|
|
Drug name Ending / Category TCA
|
-triptyline or -ipramine
|
|
|
Drug name Ending / Category -ipramine
|
TCA
|
|
|
Drug name Ending / Category -tropin
|
Pituitary hormone
|
|
|
Drug name Ending / Category Pituitary hormone
|
-tropin
|
|
|
Drug name Ending / Category -zosin
|
α1 antagonist
|
|
|
Drug name Ending / Category α1 antagonist
|
-zosin
|
