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Pharmacology Flashcards

1
Q

Km

A

Potency. It is inversely related to the affinity of the enzymes for its substrate. Km= [S] at 1/2 Vmax. The high Km, the lower the affinity.

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2
Q

Vmax

A

Efficacy. Vmax represents the maximum rate achieved by the system, at maximum (saturating) substrate concentrations.

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3
Q

Michaelis-Menten kinetics

A

Enzymatic reactions that follow a hyperbolic curve when velocity is plotted against [S]. Enzymatic reactions that exhibit a sigmoid curve usually indicate cooperative kinetics (ie hemoglobin).

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4
Q

Lineweaver-Burk plot

A

1/V plotted against 1/[S]. Y-intercept= 1/Vmax, an increase in the y-intercept = a decrease in Vmax. X-intercept= -1/Km, the closer to zero, the bigger Km is and the smaller affinity is.

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5
Q

Competitive reversible inhibitors

A

There structure resembles the substrate and binds active site of the enzyme. It can be over come by an increase in [S]. There is no effect on Vmax. It increases Km, which decreases the potency.

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6
Q

Competitive irreversible inhibitors

A

There structure resembles the substrate but does not bind the active site of the enzyme. It can not be over come by an increase in [S]. It decreases Vmax, which decreases efficacy. There is no effect on Km.

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7
Q

Noncompetitive inhibitors

A

They do not resemble substrate and do not bind the active site. It can not be overcome with an increase in [S]. It decreases Vmax, which decreases efficacy. There is no effect on Km.

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8
Q

Bioavailability (F)

A

Fraction of administered drug reaching systemic circulation unchanged. For an IV dose, F=100%. Orally, F is less than 100% due to incomplete absorption and first pass metabolism.

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9
Q

Volume of distribution (Vd)

A

Theoretical volume occupied by the total amount of drug in the body relative to its plasma concentration. Apparent Vd of plasma protein-bound drugs can be altered by liver and kidney disease (a decrease in protein binding leads to an increase in Vd). Drugs may distribute in more than one compartment. Vd=amount of drug in the body/ plasma drug concentration.

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10
Q

Low Vd

A

Usually the compartment is blood. Drug types are usually large/ charged molecules and plasma bound.

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11
Q

Medium Vd

A

Usually the compartment is ECF. Drug types are small hydrophilic molecules.

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12
Q

High Vd

A

Usually can saturate all tissues, including fat. Drug types are usually small lipophilic molecules, especially if bound to tissue protein.

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13
Q

Clearance (CL)

A

The volume of plasma cleared of drug per unit time. Clearance may be impaired with defects in cardiac, hepatic, or renal function. CL= rate of elimination of drug/ plasma drug concentration= Vd x Ke (elimination constant).

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14
Q

Half-life (t1/2)

A

The time required to change the amount of drug in the body by 1/2 during elimination (or constant infusion). Property of first order elimination. A drug infused at a constant rate takes 4-5 half-lives to reach a steady state. It takes 3.3 half lives to reach 90% of the steady state level. t1/2=(0.693 x Vd)/ CL. Time to steady state depends primarily on t1/2 and is independent of dose and dosing frequency.

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15
Q

Loading dose

A

Loading dose= (Cp x Vd)/F. Cp= target plasma concentration at steady state.

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16
Q

Maintenance dose

A

Maintenance dose= (Cp x CL x t)/ F. Cp=target dose, CL= clearance, t= dosage interval (time between doses), if not administered continuously. Cp= target plasma. In renal or liver disease, maintenance dose decreases and loading dose is usually unchanged.

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17
Q

Zero- order elimination

A

Rate of elimination is constant regardless of Cp (target plasma); constant amount of drug eliminated per unit of time. Cp decreases linearly with time. Examples of drugs include (PEA- round haped like the 0 in zero-order) Phenytoin, Ethanol, and Aspirin (at high or toxic concentrations). Capacity limited elimination.

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18
Q

First order elimination

A

Rate of elimination is directly proportional to the drug concentration (ie constant fraction of drug eliminated per unit of time). Cp decreases exponentially with time. It is flow dependent elimination.

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19
Q

Urine pH and drug elimination

A

Ionized species are trapped in urine and cleared quickly. Neutral forms can be reabsorbed. Weak acids, such as phenobarbital, methotrexate, aspirin and TCAs, get trapped in basic environment. Therefore you can treat overdoses with bicarbonate. Weak bases include amphetamines, which get trapped in acidic environments. Treat overdose with ammonium chloride.

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20
Q

Phase I drug metabolism

A

Reduction, oxidation, hydrolysis with cytochrome P-450 usually yield slightly polar, water-soluble metabolites (often still active). Geriatric patients lose phase I first.

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21
Q

Phase II drug metabolism

A

Conjugation (Glucuronidation, Acetylation, Sulfation- GAS) usually yields very polar, inactive metabolites (renally excreted). Patients who are slow acetylators have an increase in side effects from certain drugs because of a decrease in rate of metabolism.

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22
Q

Efficacy

A

The maximal effect a drug can produce. It is represented by the y-value (Vmax). It is unrelated to potency (ie efficacious drugs can have high or low potency). Partial agonists have less efficacy than full agonists.

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23
Q

Potency

A

The amount of drug needed for a given effect. An increase in potency (EC50-the concentration of a drug that gives half-maximal response)= a decrease in potency. Unrelated to efficacy (ie potent drugs can have a high or low efficacy).

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24
Q

Competitive antagonist

A

They shifts curve right (a decrease in potency, Km), no change in efficacy. Can be overcome by an increase in the concentration of agonist substrate. For example, diazepam is an agonist, while flumazenil is a competitive antagonist on the GABA receptor.

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25
Q

Noncompetitive antagonist

A

They shift the curve down, a decrease in efficacy. It cannot be overcome by an increase in agonist substrate concentration. For example, norepinephrine is an agonist, while phenoxybenzamine is a noncompetitive antagonist on alpha receptors.

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26
Q

Partial agonist (alone)

A

They act at the same site as a full agonist, but with lower than maximal effect, which is a decrease in efficacy (Vmax). Potency is an independent variable. For example, morphine is a full agonist, while buprenorphine is a partial agonistat opiod at mu-receptors.

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27
Q

Therapeutic index

A

A measurement of drug safety. TD50/ED50=median toxic dose/median effective dose= therapeutic index. Safer drugs have a higher TI value. Drugs with a lower TI value include digoxin, lithium, theophylline, and warfarin. LD50 (lethal median dose) often replaces TD50 in animal studies.

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28
Q

Therapeutic window

A

A measure of clinical drug effectiveness for a patient.

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29
Q

Botulinum toxin

A

prevents the release of acetylcholine at cholinergic terminals.

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30
Q

Nicotinic ACh receptors

A

They are ligand gated Na/K channels. Subtypes include Nn (found in autonomic ganglia) and Nm (found in neuromuscular junction).

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31
Q

Voluntary motor nerve

A

It is a somatic nerve. Lower motor neurons synapse on skeletal muscles, releasing the neurotransmitter acetylcholine, which synapse on nicotinic receptors.

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32
Q

Muscarinic ACh preceptos

A

They are G protein coupled receptors that usually act through secondary messengers. The 5 subtypes include M1, M2, M3, M4, and M5.

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33
Q

alpha-1 androgenic receptors

A

It is a Gq-protein linked 2nd messengers. It increases vascular smooth muscle contraction, increases pupillary dilator muscle contraction (mydriases), increases intestinal and bladder sphincter muscle contraction.

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34
Q

alpha-2 androgenic receptors

A

It is a Gi-protein linked 2nd messengers. It decreases sympathetic outflow, decreases insulin release, decreases lipolysis. increases platelet aggregation, and decreases aqueous humor production.

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35
Q

beta-1 androgenic receptors

A

It is a Gs-protein linked 2nd messengers. It increases heart rate, increases contractility, increases renin release, and increases lipolysis

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36
Q

beta-2 androgenic receptors

A

It is a Gs-protein linked 2nd messengers. It causes vasodilation, causes bronchodilation, increases lipolysis, increases insulin release, decreases uterine tone (tocolysis), causes ciliary muscle relaxation, and increases aqueous humor production

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37
Q

M1 receptors

A

It is a Gq-protein linked 2nd messengers. It is located in the CNS and in the enteric nervous system.

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38
Q

M2 receptors

A

It is a Gi-protein linked 2nd messengers. It decreases heart rate and contractility of atria.

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39
Q

M3 receptors

A

It is a Gq-protein linked 2nd messengers. It increases exocrine gland secretions (eg lacrimal, salivary, gastric acid), increases gut peristalsis, increases bladder contraction, causes bronchoconstriction, increases pupillary sphincter muscle contraction (miosis), causes ciliary muscle contraction (accommodation).

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40
Q

D1 receptors

A

It is a Gs-protein linked 2nd messengers. It relaxes renal vascular smooth muscle.

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41
Q

D2 receptors

A

It is a Gi-protein linked 2nd messengers. It modulates transmitter releases, especially in the brain.

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42
Q

H1 receptors

A

It is a Gq-protein linked 2nd messengers. It increases nasal and bronchial mucus production, increases vascular permeability, causes contraction of bronchioles, causes pruritus, and causes pain.

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43
Q

H2 receptors

A

It is a Gs-protein linked 2nd messengers. It increases gastric acid secretion.

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44
Q

V1 receptors

A

It is a Gq-protein linked 2nd messengers. It increases vascular smooth muscle contraction.

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45
Q

V2 receptors

A

It is a Gs-protein linked 2nd messengers. It increases H2O permeability and reabsorption in collecting tubules of the kidney (V2 found in 2 kidneys).

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46
Q

Gq receptors

A

H1, alpha1, V1, M1, M3 (HAVe 1 M&M, or 3). Binding the receptor activates phospholipase C, which cleaves PIP2 into DAG (which activates protein kinase C) and IP3 (which increases Ca, leading to smooth muscle contraction).

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47
Q

Gs receptors

A

beta1, beta2, D1, H2, V2. Gs activates adenyly cyclase, turning ATP to cAMP, which activates Protein kinase A, increasing Ca concentration (in the heart) and activating myosin light-chain kinase (in smooth muscle).

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48
Q

Gi receptors

A

M2, alpha2, D2 (MAD 2’s). Gi inhibits adenyly cyclase, reducing cAMP, inhibiting protein kinase A, decreasing Ca concentration (in the heart) and inhibiting myosin light-chain kinase (in smooth muscle).

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49
Q

Anticholinergic drug that inhibit choline reuptake in the presynaptic neuron

A

Hemicholinium

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50
Q

Anticholinergic drug that inhibit ACh uptake into vesicles in the presynaptic neuron

A

Vesamicol

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51
Q

Anticholinergic drug that inhibit ACh release from presynaptic neuron

A

Botulinum

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52
Q

Cholinergic drug that inhibit break down of ACh in synaptic cleft

A

ACh esterase inhibitors

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53
Q

Antiadrenergic drug that inhibits the conversion of tyrosine to DOPA in presynaptic neurons

A

Metryosine

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54
Q

Antiadrenergic drug that inhibits vesicular transport of norepinephrine, serotonin, and dopamine in presynaptic neurons

A

Reserpine

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55
Q

Antiadrenergic drug that blocks the release of noradrenaline from nerve terminals in presynaptic neurons

A

Bretylium

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56
Q

Antiadrenergic drug that reduces the release of catecholamines from nerve terminals in presynaptic neurons

A

Guanethidine

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57
Q

Adrenergic drugs that induce amphetamine and ephedrine from nerve terminals in presynaptic neurons

A

Amphetamine and ephedrine

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58
Q

Antiadrenergic drug that inhibit reuptake of catacholines into presynaptic neurons

A

Cocaine, TCAs, and amphetamine

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59
Q

Modulation of norepinephrine release from sympathetic nerve endings

A

It is inhibited by norepinephrine itself, acting on presynaptic alpha2- receptors

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60
Q

Bethanechol

A

Used for postoperative ileus, neurogenic ileus, and urinary retention. Direct cholinergic agonist. It activates Bowel and Bladder smooth muscle; resistant to AChE. (Bethany, call (bethanechol) me to activate your Bowels and Bladders)

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61
Q

Carbachol

A

Direct cholinergic agonist. Constricts pupil and relieves intraocular pressure in glaucoma. CARBon copy of acetylCHOLine

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62
Q

Methacholine

A

Direct cholinergic agonist. Challenge test for diagnosis of asthma. Stimulates Muscarinic receptors in airway when inhaled.

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63
Q

Pilocarpine

A

Direct cholinergic agonist. Potent stimulator of sweat, tears, and saliva. Used to treat both open angle and closed angle glaucoma. It contracts ciliary muscle of the eye (open angle glaucoma), pupillary sphincter (closed angle glaucoma). It is resistant to AChE. (You cry, drool, and sweat on your PILOw)

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64
Q

Donepezil

A

Anticholinesterases (indirect agonists). Used to treat Alzheimer disease. Increases ACh.

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65
Q

Galantamine

A

Anticholinesterases (indirect agonists). Used to treat Alzheimer disease. Increases ACh.

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66
Q

Rivastigmine

A

Anticholinesterases (indirect agonists). Used to treat Alzheimer disease. Increases ACh.

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67
Q

Edrophonium

A

Anticholinesterases (indirect agonists). Historically, used to diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab (anti-acetylcholine receptor antibody) test. Increases ACh.

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68
Q

Neostigmine

A

Anticholinesterases (indirect agonists). Postoperative and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postoperative). Increases ACh. Neo CNS= No CNS penetration.

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69
Q

Physostigmine

A

Anticholinesterases (indirect agonists). Can cause anticholinergic toxicity; it can cross blood-brain barrier into the CNS. Increases ACh. PHYsostigmine “PHYxes” atropine overdose.

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70
Q

Pyridostigmine

A

Anticholinesterases (indirect agonists). Myasthenia gravis (long acting); does not penetrate CNS. Increases ACh; increases muscle strength. PyRIDostiGMine gets RID of Myasthenia Gravis.

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71
Q

Toxicity of all cholinomimetic agents

A

Watch for exacerbation of COPD, asthma, and peptic ulcers when treating susceptible patients.

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72
Q

Cholinesterase inhibitor poisoning

A

Often due to to organophosphates, such as parathion, that irreversible inhibit AChE. Causes Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation of skeletal muscle and CNS, Lacrimation, Sweating, and Salivation. DUMBBELSS. Organophosphates are often components of insecticides; poisoning usually seen in farmers.

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73
Q

Treatment of cholinesterase inhibitor poisoning

A

Atropine (competitive inhibitor) plus pralidoxime (regenerates AChE if given early).

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74
Q

Atropine

A

Muscarinic antagonists. Targets the eye. Produces mydriasis and cycloplegia.

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75
Q

Homatropine

A

Muscarinic antagonists. Targets the eye. Produces mydriasis and cycloplegia.

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76
Q

Tropicamide

A

Muscarinic antagonists. Targets the eye. Produces mydriasis and cycloplegia.

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77
Q

Benztropine

A

Muscarinic antagonists. Targets the CNS. Treats PARKinson disease (PARK my BENZ). Also treats acute dystonia.

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78
Q

Glycopyrrolate

A

Muscarinic antagonists. Targets the GI and respiratory systems. It is used parenterally, preoperatively, to reduce airway secretions. It is also used orally, to reduce drooling and peptic ulcer.

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79
Q

Hyoscyamine

A

Muscarinic antagonists. Targets the GI system. It is used as an antispasmodics for irritable bowel syndrome.

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80
Q

Dicyclomine

A

Muscarinic antagonists. Targets the GI system. It is used as an antispasmodics for irritable bowel syndrome.

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81
Q

Ipratropium

A

Muscarinic antagonists. Targets the respiratory system. Used to treat COPD, asthma (I PRAy i can breathe soon!)

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82
Q

Tiotropium

A

Muscarinic antagonists. Targets the respiratory system. Used to treat COPD, asthma.

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83
Q

Oxybutynin

A

Muscarinic antagonists. Targets the genitourinary system. It reduces bladder spasms and urge urinary incontinence (overactive bladder).

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84
Q

Solifenacin

A

Muscarinic antagonists. Targets the genitourinary system. It reduces bladder spasms and urge urinary incontinence (overactive bladder).

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85
Q

Tolterodine

A

Muscarinic antagonists. Targets the genitourinary system. It reduces bladder spasms and urge urinary incontinence (overactive bladder).

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86
Q

Scopolamine

A

Muscarinic antagonists. Targets the CNS system. It used to treat motion sickness.

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87
Q

Atropine

A

Muscarinic antagonist. Used to treat bradycardia and for ophthalmic applications. It blocks DUMBBeLSS. Skeletal muscle and CNS excitation is mediated by nicotinic receptors. In the eyes, it increases pupil dilation and increases cycloplegia (paralysis of the ciliary muscle of the eye, resulting in a loss of accommodation). In the airway, it decreases secretions. In the stomach, it decreases acid secretions. In the gut, it decreases motility. In the bladder, it decreases urgency in cystitis.

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88
Q

Toxicity of atropine

A

Causes an increase in body temperature (due to a decrease in sweating); rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation. Can cause acute angle-closure glaucoma in elderly (due to mydriasis), urinary retention in men with prostatic hyperplasia, and hyperthermia in infants. Hot as a hare, dry as a bone, red as a beet, blind as a bat, and mad as a hatter. Jimson weed (Datura) causes gardener’s pupil (mydriasis due to plant alkaloids).

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89
Q

Tetrodotoxin

A

It is a highly potent toxin that binds fast voltage-gated Na channels in cardiac and nerve tissue, preventing depolarization (blocks action potential without changing resting potential). It causes nausea, diarrhea, paresthesias, weakness, dizziness, and loss of reflexes. Poisoning can result from ingestion of poorly prepared pufferfish (fugu), a delicacy in Japan. Treatment is primarily supportive.

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90
Q

Ciguatoxin

A

It causes ciguatera fish poisoning. It opens Na channels causing depolarization. Symptoms easily confused with cholinergic poisoning. Temperature-related dysesthesia (eg cold feels hot; hot feels cold) is a specific finding of ciguatera. It is caused by consumption of reef fish (eg barracuda, snapper, moray eel). Treatment is primarily supportive.

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91
Q

Scombroid poisoning

A

It is caused by consumption of dark-meat fish (eg bonito, mackerel, mahi-mahi, tuna) improperly stored at warm temperature. Bacterial histidine decarboxylase converts histidine to histamine. Histamine is not degraded by cooking. It is frequently misdiagnosed as an allergy to fish. It causes acute-onset burning sensation of the mouth, flushing of face, erythema, urticaria, pruritus, and headache. It may cause anaphylaxis-like presentation (ie bronchospasm, angioedema, hypotension). It is treated supportively with antihistamines; if needed, antianaphylactics (eg bronchodilators and epinephrine).

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92
Q

Albuterol

A

Direct sympathomimetics. Acts on beta2 more than beta1. Albuterol is used for acute asthma.

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93
Q

Salmeterol

A

Direct sympathomimetics. Acts on beta2 more than beta1. It is used for long term asthma and COPD control.

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94
Q

Dobutamine

A

Direct sympathomimetics. Acts on beta1 more than beta2 and alpha receptors. It is used to treat heart failure (inotropic- contraction more than chronotropic- HR), and cardiac stress test.

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95
Q

Epinephrine

A

Direct sympathomimetics. Acts on beta more than alpha receptors. It is used to treat anaphylaxis, asthma, open-angle glaucoma; alpha effects predominate at high doses. Significantly stronger effect at beta2 receptor than norepinephrine.

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96
Q

Dopamine

A

Direct sympathomimetics. Acts on D1 and D2 more than beta more than alpha. It is used to treat unstable bradycardia, HF, shock; inotropic and chronotropic alpha effects predominate at high doses.

97
Q

Isoproterenol

A

Direct sympathomimetics. Acts on beta 1 and beta 2 equally. It is used for electrophysiologic evaluation of tachyarrhythmias. Can worsen ischemia.

98
Q

Norepinephrine

A

Direct sympathomimetics. Acts on alpha 1 more than alpha 2 more than beta 1. It is used to treat hypotension (but decreases renal perfusion). It has significantly weaker effect at beta 2 receptor than epinephrine.

99
Q

Phenylephrine

A

Direct sympathomimetics. Acts on alpha1 more than alpha2. Used to treat hypotension (vasoconstriction), for ocular procedures (mydriatic), and to treat rhinitis (decongestant).

100
Q

Amphetamine

A

Indirect sympathomimetics. It as indirect general agonist, reuptake inhibitor, also releases stored catecholamines. It is used to treat narcolepsy, obesity, and ADHD.

101
Q

Cocaine

A

Indirect sympathomimetics. It as indirect general agonist, reuptake inhibitor. It causes vasoconstriction and local anesthesia. Never give a beta blocker if there is a cocaine intoxication is suspected (can lead to unopposed alpha1 activation and extreme hypertension).

102
Q

Ephedrine

A

Indirect sympathomimetics. It as indirect general agonist, releases stored catecholamines. It is used to treat nasal decongestion, urinary incontinence, and hypotension.

103
Q

Norepinephrine vs isoproterenol

A

Norepinephrine increases systolic and diastolic pressures as a result of alpha-1 mediated vasoconstriction, leading to an increase in mean arterial pressure, which causes reflex bradycardia. However, isoproterenol (no longer commonly used) has little alpha effect but causes beta-2 mediated vasodilation, resulting in a decrease in mean arterial pressure and an increase in heart rate through beta-1 and reflex activity.

104
Q

Clonidine applications

A

Sympatholytics (alpha2 agonists). It is used for hypertensive urgency (limited situations); it does not decrease renal blood flow. It is also used to treat ADHD and tourette syndrome. Toxicities include CNS depression, bradycardia, hypotension, respiratory depression, and miosis.

105
Q

alpha methyldopa

A

Sympatholytics (alpha2 agonists). It is used for hypertension in pregnancy. Toxicities direct Coombs positive hemolysis, SLE-like syndrome.

106
Q

Phenoxybenzamine

A

Irreversible alpha blocker. Used to treat pheochromocytoma (used preoperatively) to prevent catecholamine (hypertensive) crisis. Side effects include orthostatic hypotension and reflex tachycardia.

107
Q

Phentolamine

A

Reversible alpha blocker. Used to give to patients on MAO inhibitors who eat tyramine containing foods. Side effects include orthostatic hypotension and reflex tachycardia.

108
Q

Prazosin

A

Alpha 1 selective blocker. It is used for urinary symptoms of BPH; it is also used to treat PTSD and hypertension. Side effects include 1st dose orthostatic hypotension, dizziness, and headache.

109
Q

Terazosin

A

Alpha 1 selective blocker. It is used for urinary symptoms of BPH. Side effects include 1st dose orthostatic hypotension, dizziness, and headache.

110
Q

Doxazosin

A

Alpha 1 selective blocker. It is used for urinary symptoms of BPH; it is also used to treat hypertension. Side effects include 1st dose orthostatic hypotension, dizziness, and headache.

111
Q

Tamsulosin

A

Alpha 1 selective blocker. It is used for urinary symptoms of BPH; it is also used to treat hypertension. Side effects include 1st dose orthostatic hypotension, dizziness, and headache.

112
Q

Mirtazapine

A

Alpha 2 selective blocker. It is used to treat depression. Side effects include sedation, an increase in serum cholesterol, and an increase appetite.

113
Q

alpha blockade with epinephrine vs phenylephrine

A

When an alpha blockage is given after epinephrine or phenylephrine. The epinephrine response exhibits reversal of the mean blood pressure changes, from a net increase (the alpha response) to a net decrease (the beta2 response). The response to phenylephrine is suppressed but not reversed because phenylephrine is a pure alpha agonist without beta action.

114
Q

Beta blockers

A

Acebutolol, atenolol, betaxolol, carvedilol, esmolol, labetalol, metoprolol, nadolol, nebivolol, pindolol, timolol.

115
Q

Beta blockers application towards angina pectoris

A

beta blockers decrease heart rate and contractility, resulting in a decrease in O2 consumption.

116
Q

Beta blockers application towards MI

A

Beta blockers (metoprolol, carvedilol, and bisoprolol) decreases mortality.

117
Q

Beta blockers application towards supraventricular tachycardia

A

Metoprolol and esmolol decrease AV conduction velocity (class II antiarrhythmic)

118
Q

Beta blockers application towards hypertension

A

They decrease cardiac output, decrease renin secretion (due to beta1 receptor blockade on JGA cells)

119
Q

Beta blockers application towards heart failure

A

they decrease chronic HF

120
Q

Beta blockers application towards glaucoma

A

timolol decreases secretion of aqueous humor.

121
Q

Toxicity of beta blockers

A

They can cause impotence, cardiovascular adverse effects (bradycardia, AV block, HF), CNS adverse effects (seizures, sedation, and sleep alterations), dyslipidemia (metoprolol), and asthma/COPD exacerbations. Avoid in cocaine users due to risk of unopposed alpha adrenergic receptor agonist activity. Despite theoretical concern of masking hypoglycemia in diabetics, benefits likely outweigh risks and is not containdicated.

122
Q

beta1 antagonists

A

Acebutolol (partial agonist), atenolol, betaxolol, esmolol, metroprolol. Selective antigonists mostly go from A to M (Beta 1 with the 1st half of the alphabet)

123
Q

Nonselective beta agonists

A

Nadolol, pindolol (partia agonist), propranolol, timolol. Nonseletive antagonists mostly go from N to Z.

124
Q

Carvedilol

A

Nonselective alpha and beta antagonists.

125
Q

Labetalol

A

Nonselective alpha and beta antagonists.

126
Q

Nebivolol

A

Combines cardiac selective beta1 adrenergic blockade with stimulation of beta3 receptors, which activate nitric oxide synthase in the vasculature.

127
Q

Antidote for acetaminophen overdose

A

N-acetylcysteine (replenishes glutathione)

128
Q

Antidote for AChE inhibitors and organophosphates overdose

A

Atropine works better than pralidoxime

129
Q

Antidote for amphetamines (basic) overdose

A

NH4Cl acidifies the urine

130
Q

Antidote for antimuscarinic and anticholinergic overdose

A

Physostigmine salicylate and control hyperthermia

131
Q

Antidote for benzodiazepines overdose

A

Flumazenil

132
Q

Antidote for beta-blockers overdose

A

glucagon

133
Q

Antidote for carbon monoxide overdose

A

100% O2, hyperbaric O2

134
Q

Antidote for coper overdose

A

Penicillamine

135
Q

Antidote for arsenic overdose

A

Penicillamine

136
Q

Antidote for gold overdose

A

Penicillamine

137
Q

Antidote for cyanide overdose

A

Nitrate plus thiosulfate or hydroxocobalamin

138
Q

Antidote for digitalis (digoxin) overdose

A

Anti-dig Fab fragments

139
Q

Antidote for heparin overdose

A

Protamine sulfate

140
Q

Antidote for iron overdose

A

DFEroxamine or deFErasirox

141
Q

Antidote for lead overdose

A

EDTA, dimercaprol, succimer, or penicillamine

142
Q

Antidote for mercury overdose

A

DiMERCaprol (BAL) or succimer

143
Q

Antidote for arsenic overdose

A

Dimercaprol (BAL) or succimer

144
Q

Antidote for gold overdose

A

Dimercaprol (BAL) or succimer

145
Q

Antidote for methanol or ethylene glycol (antifreeze) overdose

A

Fomepizole works better than ethanol. Dialysis is also an option.

146
Q

Antidote for methemoglobin overdose

A

METHyleneblue or vitamin C

147
Q

Antidote for opioids overdose

A

Naloxone or naltrexone

148
Q

Antidote for salicylates overdose

A

NaHCO3 (alkalinize urine) or dialysis

149
Q

Antidote for TCAs overdose

A

NaHCO3 (plasma alkalinization)

150
Q

Antidote for tPA overdose

A

Aminocaproic acid

151
Q

Antidote for streptokinase overdose

A

Aminocaproic acid

152
Q

Antidote for urokinase overdose

A

Aminocaproic acid

153
Q

Antidote for warfarin overdose

A

Vitamin K (delayed effect) or fresh frozen plasma (immediate effect)

154
Q

Drug reactions causing coronary vasospasm

A

Cocaine, sumatriptan, ergot alkaloids

155
Q

Drug reactions causing cutaneous flushing

A

Vancomycin, Adenosine, Niacin, Ca channel blockers (VANC)

156
Q

Drug reactions causing dilated cardiomyopathy

A

Anthracyclines (eg doxorubicin, daunorubicin), can be prevented with dxrazoxane

157
Q

Drug reactions causing torsades de pointes

A

Class III (eg sotalol) and class IA (eg quinidine) antiarrhythmics, macrolide antibiotics, antipsychotics, TCAs

158
Q

Drug reactions causing adrenocortical insufficiency

A

Hypothalamic–pituitary–adrenal axis (HPA axis) secondary to glucocorticoid withdrawal.

159
Q

Drug reactions causing hot flashes

A

Tamoxifen, clomiphene

160
Q

Drug reactions causing hyperglycemia

A

Tacrolimus, Protease inhibitors, Niacin, Hydrochlorothiazide (HCTZ), Corticosteroids (Taking Pills Necessitates Having blood Checked)

161
Q

Drug reactions causing hypothyroidism

A

Lithium, amiodarone, sulfonamides

162
Q

Drug reactions causing acute cholestatic hepatitis and jaundice

A

Erthromycin

163
Q

Drug reactions causing diarrhea

A

Metformin, Erythromycin, Colchicine, Orlistat, Acarbose (Might Excite Colon On Accident)

164
Q

Drug reactions causing focal to massive hepatic necrosis

A

Halothane, Amanita phalloides (death cap mushroom), Valproic acid, Acetaminophen (liver HAVAc)

165
Q

Drug reactions causing hepatitis

A

Rifampin, isoniazid, pyrazinamide, statins, fibrates.

166
Q

Drug reactions causing pancreatitis

A

Didanosine, Corticosteroids, Alchol, Valproic acid, Azathioprine, Diuretics (furosemide, HCTZ) (Drugs Causing A Violent Abdominal Distress)

167
Q

Drug reactions causing pseudomembranous colitis

A

Clindamycin, ampicillin, caphalosporins. (antibiotics predispose to superinfection by resistant C difficle.

168
Q

Drug reactions causing agranulocytosis

A

Ganciclovir, Clozapine, Carbamazepine, Colchicine, Methimazole, Propylthiouracil (Gangs CCCrush Myeloblasts and Promyelocytes)

169
Q

Drug reactions causing aplastic anemia

A

Carbamazepine, Methimazole, NSAIDs, Benzene, Chloramphenicol, Propylthiouracil (Can’t Make New Blood Cells Properly)

170
Q

Drug reactions causing direct Coombs-positive hemolytic anemia

A

Methylodopa, penicillin

171
Q

Drug reactions causing gray baby syndrome

A

Chloramphenicol

172
Q

Drug reactions causing hemolysis in G6PD deficiency

A

Isoniazid, Sulfonamides, Dapsone, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin (hemolysis IS D PAIN)

173
Q

Drug reactions causing megaloblastic anemia

A

Phenytoin, Methotrexate, Sulfa drugs (Having a blast with PMS)

174
Q

Drug reactions causing thrombocytopenia

A

Heparin

175
Q

Drug reactions causing thrombotic complications

A

OCPs, hormone replacement therapy

176
Q

Drug reactions causing fat redistribution

A

Protease Inhibitors, Glucocorticoids (Fat PIG)

177
Q

Drug reactions causing gingival hyperplasia

A

Phenytoin, Ca channel blockers, cyclosporine

178
Q

Drug reactions causing hyperuricemia (gout)

A

Pyrazinamide, Thiazides, Furosemide, Niacin, Cyclosporine (Painful Tophi and Feet Need Care)

179
Q

Drug reactions causing myopathy

A

Fibrates, niacin, colchicine, hydroxychloroquine, interferon-alpha, penicillamine, statins, glucocorticoids

180
Q

Drug reactions causing osteoporosis

A

Corticosteroids, heparin

181
Q

Drug reactions causing photosensitivity

A

Sulfonamides, Amiodarone, Tetracyclines, 5-FU (SAT for Foto)

182
Q

Drug reactions causing Stevens-Johnson syndrome

A

Anti-epileptic drugs (especially lamotrigine), allopurinol, sulfa drugs, penicillin. (Steven Johnson has epileptic ALLergy to sulfa drugs and penicillin)

183
Q

Drug reactions causing SLE-like syndrome

A

Sulfa drugs, Hydralazine, Isoniazid, Procainamide, Phenytoin, Etanercept (having lupus is “SHIPP-E”

184
Q

Drug reactions causing teeth discoloration

A

tetracyclines

185
Q

Drug reactions causing tendonitis, tendon rupture, and cartilage damage

A

Fluoroquinolones

186
Q

Drug reactions causing cinchonism

A

Quinidine, quinine

187
Q

Drug reactions causing parkinson-like syndrome

A

Antipsychotics, Reserpine, Metoclopramide (cogwheel rigidity of ARM)

188
Q

Drug reactions causing seizures

A

Isoniazid (due to vitamin B6 deficiency), Bupropion, Imipenem/cilastatin, Enflurane (With seizures, I BItE my tongue)

189
Q

Drug reactions causing tardive dyskinesia

A

Antipsychotics, metoclopramide

190
Q

Drug reactions causing diabetes insipidus

A

Lithium, demeclocycline

191
Q

Drug reactions causing Fanconi syndrome

A

Expired tetracycline

192
Q

Drug reactions causing hemorrhagic cystitis

A

Cyclophosphamide, ifosfamide (prevent by coadministering with mesna)

193
Q

Drug reactions causing interstitial nephritis

A

Methicillin, NSAIDs, furosemide

194
Q

Drug reactions causing SIADH

A

Carbamazepine, Cyclophosphamide, SSRIs (Can’t Concentrate Serum Sodium)

195
Q

Drug reactions causing dry cough

A

ACE inhibitors

196
Q

Drug reactions causing pulmonary fibrosis

A

Bleomycin, Amiodarone, Busulfan, Methotrexate (Breathing Air Badly from Medications)

197
Q

Drug with antimuscarinic reactions

A

Atropine, TCAs, H1-blockers, antipsychotics

198
Q

Drug reactions causing a disulfiram like reaction

A

Metronidazole, certain cephalosporins, griseofulvin, procarbazine, 1st generation sulfonylureas

199
Q

Drug reactions causing nephrotoxicity/ototoxicity

A

Aminoglycosides, vancomycin, loop diuretics, cisplatin. Cisplatin toxicity may respond to amifostine

200
Q

Cytochrome P-450 inducers

A

Chronic alcohol use, St John’s wort, Phenytoin, Phenobarbital, Nevirapine, Rifampin, Griseofulvin, Carbamazepine (Chronic alcoholics STeal Phen-PHen and Never Refuse Greasy Carbs.

201
Q

Cytochrome P-450 substrates

A

Anti-epileptics, Theophylline, Warfarin, OCPs (Always Think When Outdoors)

202
Q

Cytochrome P-450 inhibitors

A

Acute alcohol abuse, Ritonavir, Amiodarone, Cimetidine, Ketoconazole, Sulfonamides, Isoniazid (INH), Grapefruit juice, Quinidine, Macrolides (except azithromycin) (AAA RACKS IN GQ Magazine)

203
Q

Sulfa drugs

A

Probenecid, Furosemide, Acetazolamide, Celecoxib, Thiazides, Sulfonamide antibiotics, Sulfasalazine, Sulfonylureas. (Popular FACTSSS) Patients with sulfa allergies may develop fever, urinary tract infection, Stevens-Johnson syndrome, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria (hives). Symptoms range from mild to life threatening.

204
Q

Drugs ending with -azole

A

Ergosterol synthesis inhibitor, eg ketoconazole

205
Q

Drugs ending with -bendazole

A

Antiparasitic/antihelmintic, eg mebendazole

206
Q

Drugs ending with -cillin

A

Peptidoglycan synthesis inhibitor, eg ampicillin

207
Q

Drugs ending with -cycline

A

Protease synthesis inhibitor, eg tetracycline

208
Q

Drugs ending with -ivir

A

Neuraminidase inhibitor, eg oseltamivir

209
Q

Drugs ending with -navir

A

Protease inhibitor, eg ritonavir

210
Q

Drugs ending with -ovir

A

DNA polymerase inhibitor, eg acyclovir

211
Q

Drugs ending with -thromycin

A

macrolide antibiotic, eg azifthromycin

212
Q

Drugs ending with -ane

A

Inhalational general anesthetic, eg halothane

213
Q

Drugs ending with -azine

A

Typical antipsychotic, eg thioridazine

214
Q

Drugs ending with -barbital

A

Barbiturate, eg phenobarbital

215
Q

Drugs ending with -caine

A

Local anesthetic, eg lidocaine

216
Q

Drugs ending with -etine

A

SSRI, eg fluoxetine

217
Q

Drugs ending with -ipramine or -triptyline

A

TCA, eg imipramine, amitriptyline

218
Q

Drugs ending with -triptan

A

5-HT1B/1D agonists, sumatriptan

219
Q

Drugs ending with -zepam or -zolam

A

Benzodiazepine, eg diazepam or alprazolam

220
Q

Drugs ending with -chol

A

Cholinergic agonist, eg bethanechol/carbachol

221
Q

Drugs ending with -curium or -curonium

A

Nondepolarizing paralytic, eg atracurium, vecuronium

222
Q

Drugs ending with -olol

A

beta-blocker, eg propranolol

223
Q

Drugs ending with -stigmine

A

AChE inhibitor, neostigmine

224
Q

Drugs ending with -terol

A

beta2-agonist, eg albuterol

225
Q

Drugs ending with -zosin

A

alpha1-antagonist, eg prazosin

226
Q

Drugs ending with -afil

A

PDE-5 inhibitor, eg sildenafil

227
Q

Drugs ending with -dipine

A

Dihydropyridine CCB, eg amlodipine

228
Q

Drugs ending with -pril

A

ACE inhibitor, eg captopril

229
Q

Drugs ending with -sartan

A

Angiotensin-II receptor blocker, eg losartan

230
Q

Drugs ending with -statin

A

HMG-CoA reductase inhibitor, eg atorvastatin

231
Q

Drugs ending with -dronate

A

Bisphosphonate, eg alendronate

232
Q

Drugs ending with -glitazone

A

PPAR-gamma activator, eg rosiglitazone

233
Q

Drugs ending with -prazole

A

Proton pump inhibitor, eg omeprazole

234
Q

Drugs ending with -prost

A

Prostaglandin analog, eg latanoprost

235
Q

Drugs ending with -tidine

A

H2-antagonist, eg cimetidine

236
Q

Drugs ending with -tropin

A

Pituitary hormone, eg somatotropin

237
Q

Drugs ending with -ximab

A

Chimeric monoclonal Ab, basiliximab

238
Q

Drugs ending with -zumab

A

Humanized monoclonal, eg daclizumab

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