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Boards Review by Topic > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Captopril class

A

ACE inhibitor

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2
Q

Verapamil class

A

Ca channel blocker

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3
Q

Brimonidine (Alphagan)

A

Alpha 2 agonist

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4
Q

Bethanechol (Urecholine)

A

Direct acting cholinergic agonist

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5
Q

Methylphenidate (Ritalin)

A

Stimulant used in ADHD

Same function as amphetamine

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6
Q

Betaxolol (Betoptic)

A

Beta-1 Blocker

1 blocker; tx glaucoma in asthmatics; Tx: HTN and angina

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7
Q

When are beta blockers used?

A

Acute MI, CHF, HTN, arrhythmia, angina

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8
Q

Cocaine

A

Inhibits DA and NE re-uptake into terminals has amphetamine-like effect but shorter acting and more intense
Severe HTN and stroke, tachycardia
Used for nasal surgery to decrease blood flow

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9
Q

Succinylcholine (Anectine)

A

Depolarizing NMJ Blocker
initial stimulation and contraction→blockade; rapid procedures;
Phase I –prolonged depolarization, NO Reversal w/ AchE inh., makes it worse;
Phase II:AchE inh works;
SE: hypercalcemia, hyperkalemia-K+release(cardiac arrest – in burn/trauma pts), muscle pain

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10
Q

Amlodipine class

A

Ca channel blocker

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11
Q

Phenylephrine (Neo-Synephrine: Sudafed PE)

A

Alpha agonist
α1 selective agonist; use in hypotensive emergency; produces mydriasis, nasal decongestant(rebound), contracts prostate and GU spinchters

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12
Q

Contraindications for beta blockers

A

Sinus bradycardia, heart block greater than first degree, sick sinus syndrome, cardiogenic shock, decompensated heart failure, asthma, COPD

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13
Q

Tropicamide (Mydriacil)

A

Cholinergic (muscarinic) Antagonist

short-acting mydriasis and cycloplegia for eye examinations

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14
Q

Nifedipine class

A

Ca channel blocker

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15
Q

Cisatracurium (Nimbex)

A

Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium

Most commonly used (least toxic)

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16
Q

Clonidine

A

Centrally acting alpha-2 agonist reduces sympathetic outflow and causes vasodilation and decreased CO for lower BP
selective α2 agonist; transdermal patch; tx for HTN, safe in renal disease; reduces craving in addicts, ↓ hot flashes

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17
Q

Altracurium (Tracium)

A

Non-Depolarizing NMJ Blocker

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18
Q

Nicotine

A

Direct acting cholinergic agonist

Selective for Nicotinic receptors;NMJ intial stim paralysis; Tx Atropine

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19
Q

Prazosin (Minipress)

A

Alpha-1 selective blocker
selective for α1; lack of α2 block reduces likelihood of reflex tachycardia;
Tx: BPH and HTN Tox: 1st dose orthostatic hypotension; CI: w/ Viagra

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20
Q

Terbutaline (Brethine)

A

Beta 2 agonist

Selective ß2 agonist; reduce premature uterine contractions

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21
Q

Echothiophate

A

Cholinesterase Inhibitors

instill directly into eye; tx glaucoma in emergency; long action

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22
Q

Tyramine

A

Indirectly increases release of catecholamines from nerve terminals
Replaces NE in vesicles with octopamine
Normally hydrolyzed by MOA in the gut and therefore inactive when given orally
Normal component of many foods

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23
Q

Dobutamine (Dobutrex)

A

Beta 1 agonist

selective ß1 agonist, inotropic and chronotropic; cardiac stress test, heart failure, increase renin release

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24
Q

Norepinephrine (Levophed)

A

Catecholamine
stimulate α=ß1»ß2; severe vasoconstriction at infusion site→ necrosis, tx: hypotension; effects ↑systolic, ↑diastolic ↑ MAP, no change in PP reflex ↓HR (ganglion blockers stop reflex bradycardia)
↓ = depression; pain regulation

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25
Q

Organophosphate pesticides

A

Cholinesterase Inhibitors

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26
Q

Metoprolol (Lopressor)

A

Beta-1 Blocker
1 blocker; inc. life post-MI; decrease renin; better exercise tolerance and in diabetics; risky in asthma(Use Ca++ channel blkrs in asthmatics)

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27
Q

Aliskiren class

A

Renin inhibitor

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28
Q

Carbachol (Isopto Carbachol)

A

Direct acting cholinergic agonist

Glaucoma, pupillary contraction, relieves intraocular pressure

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29
Q

Phenoxybenzamine (Dibenzyline)

A

Alpha receptor blocker
Irreversible non-competitive antagonist at α1 and α2 ;tx: pheochromocytoma use pre surgery cuz catecholamines cant overcome noncompetitive inhibitor; SE: hypotension and tachycardia

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30
Q

Phentolamine (Regitine)

A

Alpha receptor blocker
Reversible competitive antagonist at α1 and α2; tx pt on MAO-I who ingest tyramine (HTN crisis); SE: release of Histmaine from Mast cells = gastric acid secretion PUD

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31
Q

Acebutolol (sectral)

A

Beta Blocker with intrinsic sympathetic activity

selective ß1 antagonist w/ ISA; risk of bradycardia decreased

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32
Q

Glycopyrrolate (Rubinul)

A

Cholinergic (muscarinic) Antagonist
used in surgery to ↓ vagal response as well as decrease respiratory and other secretions;
Also decreases gastric acid secretion to treat PUD
Decrease side effects in tx of MG with Neostigmine and anytime Neostigmine is used after surgery

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33
Q

Albuterol (Ventolin)

A

Beta 2 agonist

selective ß2 agonist; tx asthma, relax skeletal mm BV, promote K uptake

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34
Q

Losartan class

A

ARB

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35
Q

What category of drugs are the -prils? Example: Captopril

A

ACE inhibitors
Common side effect of ACEI’s is coughing from decreased bradykinin breakdown
First line treatments for HTN in DM, Renal Disease, LVH
CI in pregnancy, causes acute renal failure in patients with renal artery stenosis, causes hyperkalemia

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36
Q

Enalapril

A

ACE inhibitor
Common side effect of ACEI’s is coughing
First line treatments for HTN in DM, Renal Disease, LVH, congestive heart failure
CI in pregnancy, causes acute renal failure in patients with renal artery stenosis, causes hyperkalemia

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37
Q

Apraclonidine (Iopidine)

A

Alpha 2 agonist

Selective α2 agonist used in eye to tx intraocular pressure by ↓ fluid

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38
Q

Donepezil (Aricept)

A

Cholinesterase Inhibitors

Alzheimer’s disease; similar drug is Tacrine(severely hepatotoxic)

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39
Q

Adverse effects of beta blockers

A

Bradycardia, dizziness, HA, fatigue, hypotension, fainting, sexual dysfunction, bronchospasm

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40
Q

Chlorthalidone

A

Thiazide diuretic

Prevents Na reabsoprtion in early distal tubule

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41
Q

Rocuronium (Zemuron)

A

Non-Depolarizing NMJ Blocker

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42
Q

Pindolol (Visken)

A

Beta Blocker with intrinsic sympathetic activity

nonselective β blocker with some ISA; Tx: HTN and angina

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43
Q

Varenicline (Chantix)

A

Direct acting cholinergic agonist

Partial agonist at Nicotinic Receptors(in the brain) N/V, Constipation, Vivid nightmares, psychosis

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44
Q

Amphetamine

A

Indirect acting sympathomimetic
Displaces NE and DA from vesicles increasing their release
CNS stimulant
Strong external urinary sphincter contractor

Releases stored catecholamines, blocks reuptake, CNS stimulant; tachycardia, HTN, psychosis ; uses : narcolepsy, obesity, ADD

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45
Q

Side effects of Clonidine

A

Centrally acting alpha-2 agonist
Hypotension, dry mouth, somnolence, fatigue, constipation, dizziness
Rebound HTN possible when discontinue use

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46
Q

Candesartan class

A

ARB

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47
Q

Pilocarpine (Isopto Carpine; Pilocar)

A

Direct acting cholinergic agonist
tx glaucoma; Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle); sweat and salivate excessively; SE; blurred vision

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48
Q

Carvedilol (Coreg)

A

Combined alpha and beta blocker

ß-blocker and α1 blocker; decreases free radicals; tx HTN/CHF, post-MI

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49
Q

Oxybutynin (Ditropan)

A

Cholinergic (muscarinic) Antagonist

prevent bladder spasm after prostate surgery

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50
Q

Diltiazem class

A

Ca channel blocker

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51
Q

What are the first line drugs used for depression?

A

SSRI’s are the first-line drugs especially for those with suicidal ideation
Examples: fluoxetine, paroxetine, citalopram, sertraline

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52
Q

Oxymetazoline (Afrin)

A

Alpha agonist

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53
Q

Neostigmine (Prostigmin)

A

Cholinesterase Inhibitors

Not X BBB; tx myasthenia gravis, post op and neurogenic ileus, reverse NMJ block

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54
Q

Tolterodine (Detrol)

A

Cholinergic (muscarinic) Antagonist

Selective M3 – tx overactive bladder

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55
Q

Propranolol (Inderol)

A

Beta-receptor blocker
non-selective competitive antagonist; tx, HTN, post-MI, angina, arrhythmias, CHF, hyperthyroidism, stage-fright; DO NOT discontinue abruptly(up-reg of receptors)

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56
Q

Ipratropium (Atrovent)

A

Cholinergic (muscarinic) Antagonist

inhalation for tx COPD and Asthma(blks Vaso-C)

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57
Q

Scopolamine

A

Cholinergic (muscarinic) Antagonist

patch tx motion sickness; Penetrates CNS; SE:sedation/amensia

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58
Q

Nebivolol (Bystolic)

A

Beta-1 Blocker

Most selective 1 blocker; Vaso-D due NO from endothelium; reduces cholesterol, TG’s and blood glucose

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59
Q

Physostigmine (Eserine)

A

Cholinesterase Inhibitors
instill directly into eye, crosses BBB; tx glaucoma, atropine poisoning
“phyxes” atropine overdose

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60
Q

Cevimeline (Evoxac)

A

Direct acting cholinergic agonist

Selective for M3 receptors – salivation Not sweating

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61
Q

Acetylcholine (Miochol)

A

Direct acting cholinergic agonist
M and N receptors
No clinical use
acts on M and N receptors; memory, cognition, attention; Ach neurons degenerate in Alzheimer’s(nucleus basalis & hippocampus); balances DA

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62
Q

Esmolol (Brevibloc)

A

Beta-1 Blocker

1 blocker very short duration of action; give IV; tx if unsure pt can handle beta blockers

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63
Q

Tetrahydrazoline (Visine)

A

Alpha agonist

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64
Q

Salmeterol (Serevent)

A

Beta 2 agonist

selective ß2 agonist; tx asthma, relax skeletal mm BV, promote K uptake

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65
Q

What category of drugs are the -sartans? Example: Losartan

A

ARB’s
Angiotensin Receptor Blockers
More specific than ACEI’s with similar side effects except for cough and angioedema

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66
Q

Dicyclomine (Bentyl)

A

Cholinergic (muscarinic) Antagonist

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67
Q

Atropine

A

Cholinergic (muscarinic) Antagonist
early MI to decrease bradycardia or AV block, cholinesterase inhibitor posining; SE: ↑pupil dilation, cycloplegia ↓airway secretion ↓gastric acid secretion ↓GI motility ↓urgency in cystitis ↑body temp (due to ↓sweating) Other SE(dose-dependent): dry mouth/skin ↑HR blurred vision/palpitations GI effects Delerium, Think “Hot as a hare, dry as a bone, red as a beet, mad as a hatter”

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68
Q

Nicardipine class

A

Ca channel blocker

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69
Q

Isoproterenol (Isuprel)

A

Catecholamine
ß1 and ß2 agonist; emergency tx of cardiac arrest (AV block) effects: no change/slight decrease in systolic, ↓diastolic, ↓MAP, reflex ↑HR

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70
Q

Epinephrine (Adrenaline)

A

Catecholamine
low dose selective for ß1 (looks like isoproterenol), high dose all adrenergic receptors; tx anaphylactic shock, cardiac arrest & complete heart blk, glaucoma; ß2 – cause Broncho-D
effects: ↑Systolic, ↓Diastolic, no change in MAP, ↑ Pulse Pressure, reflex ↑HR (due to ↓ diastolic) CI: in pts on β-Blkrs

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71
Q

Clonidine (Catapres)

A

Alpha 2 agonist

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72
Q

Mecamylamine (Inversine)

A

Ganglion Blocker
Rarely used
nicotinic agonist effects like blocking both sympathetic and parasympathetic input; prevents vagal reflex responses to changes in blood pressure, i.e. prevents reflex bradycardia caused by NE;
SE: cycloplegia, mydriasis, blurred vision, orthostatic hypotension, tachycardia, urinary retention, sexual dysfunction

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73
Q

Edrophonium (Tensilon)

A

Cholinesterase Inhibitors
binds reversibly; IV; Dx of myasthenia gravis; drug titration – strength increases to a point, then decreases; short action

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74
Q

Bethanechol

A

Cholinergic Agonist

Selective muscarinic receptors, stimulate peristalsis and urination, for post operative and neurogenic ileus

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75
Q

d-Tubocurarine

A

Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium

histamine release leads to hypotension + Bronchospasm

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76
Q

Tamsulosin (Flomax)

A

Alpha-1 selective blocker

selective for α1A; tx BPH w/ little effect on BP; SE:↓ejaculation

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77
Q

Sotalol (Betapace)

A

Beta-receptor blocker

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78
Q

Ephedrine

A

Alpha, Beta agonist and increases NE release
Similar effects to epinephrine but not as pronounced
Releases stored catecholamines, has direct action; uses: nasal decongestant, urinary incontinence, hypotension

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79
Q

Solifenacin (Vesicare)

A

Cholinergic (muscarinic) Antagonist

Selective M3 – tx overactive bladder

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80
Q

Hexamethonium

A

Ganglion Blocker
Rarely used
nicotinic agonist effects like blocking both sympathetic and parasympathetic input; prevents vagal reflex responses to changes in blood pressure, i.e. prevents reflex bradycardia caused by NE;
SE: cycloplegia, mydriasis, blurred vision, orthostatic hypotension, tachycardia, urinary retention, sexual dysfunction

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81
Q

Reserpine

A

Causes depletion of NE, DA, 5-HT

No longer used

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82
Q

Pancuronium

A

Non-Depolarizing NMJ Blocker
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium

vagal blockade and tachycardia

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83
Q

Methacholine

A

Cholinergic agonist

Dx of Asthma – stims M recetors in airway when inhaled

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84
Q

Pyridostigmine

A

Cholinesterase Inhibitor

Myasthenia gravis, long acting, does not penetrate CNS

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85
Q

Pralidoxime (2 PAM)

A

early tx organophosphate poisoning; CI: Carbamates(don’t age)

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86
Q

What are the SSx of organophosphate poisoning and how is it treated?

A

DUMBBELSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardis, Excitation of skeletal muscles and CNS, Lacrimation, Sweating, Salivation

Tx: atropine + pralidoxime (2-PAM) before the aging process

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87
Q

Methscopolamine

A

Cholinergic Antagonist

Peptic Ulcer Treatment

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88
Q

Dyphenoxylate-atropine (Lomotil)

A

Cholinergic Antagonist

Combo of opoid and atropine to treat Diarrhea

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89
Q

Benztropine

A

Cholinergic Antagonist

decrease extrapyramidal symptoms of antipsychotics; Parkinson’s

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90
Q

Vecuronium

A

Non-Depolarizing Neuromuscular Blockers
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium

liver metab; duration 20-40mins

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91
Q

Rocuronium

A

Non-Depolarizing Neuromuscular Blockers
Use: surgery- paralysis, mechanical ventilation, selective for motor nicotinic receptors, Reverse with neostigmine or edrophonium

intubation (rapid onset)

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92
Q

Dopamine

A

Catecholamine
low dose activate D1, high dose ß1 on heart; tx cardiac shock w/o VasoC
addiction, emotions, movement; Nigro-striatal DA neuron degeneration in Parkinson’s; excess = psychosis, schizophrenia

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93
Q

Alpha-methyldopa

A

Selective α2 agonist; Same as clonidine but safe in pregos

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94
Q

Ritrodine

A

Selective ß2 agonist; reduce premature uterine contractions

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95
Q

How do beta 2 receptors influence aqueous humor production?

A

Beta-2 receptors increase production of aqueous humor leading to increased IOP

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96
Q

Fendolapam

A

Selective D1 agonist; dilation of vascular beds

Tx severe HTN rapidly

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97
Q

What drug causes orange colored urine and what is it used to treat?

A

Rifampin

TB

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98
Q

What are the 4 first-line drugs for TB?

A

Isoniazid, Rifampin, Ethambutol, Pyrazinamide

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99
Q

Isoniazid

A

Treatment for TB, inhibits P450, can cause Vit B6 deficiency, hepatitis, peripheral neuropathy

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100
Q

Rifampin

A

Treatment for TB, orange colored urine, inhibits DNA dependent RNA polymerase, induces P450, hepatotoxic

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101
Q

Ethambutol

A

Treatment for TB, causes color blindness and decreased visual acuity

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102
Q

Pyrazinamide

A

Treatment for TB, causes non-gouty arthralgia

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103
Q

Common P450 inducers

A 
Rifampin
Phenobarbitol
Carbamazepine
Phenytoin
St. John's wart
Corticosteroids
Efavirenz
Pioglitazone
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104
Q

Common P450 inhibitors

A 
Isoniazid
Cimetidine
Azole antifungals
Erythromycin
Grapefruit juice
SSRI's
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105
Q

What are common toxicities from aminoglycosides like Streptomycin?

A

Ototoxicity

Nephrotoxicity

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106
Q

Terazosin, Doxazosin

A

Alpha receptor blocker
selective for α1; lack of α2 block reduces likelihood of reflex tachycardia; Tx: BPH and HTN Tox: 1st dose orthostatic hypotension; CI: w/ Viagra

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107
Q

Yohimbine

A

α2 selective antagonist; increases NE release; acts opposite Clonidine

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108
Q

Mirtazapine

A

α2 selective antagonist; use: depression w/ insomnia; SE: sedation, inc. serum cholesterol, inc. appetite

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109
Q

Timolol

A

Beta Blocker

non-selective competitive antagonist; tx glaucoma(↓ aqueous humor production; CI: asthmatics

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110
Q

Labetalol

A

Beta Blocker

blocks ß1 ß2 and α1; IV tx hypertensive emergency; SE: liver injury

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111
Q

Guanethidine

A

Replaces NE in vesicles decreasing its release

Used for HTN

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112
Q

Reserpine

A 
Antipsychotic, anti HTN
Inhibits VMAT
Decreases catecholamines
Increases cholinergic effects in body–ANS, GI, BV, smooth muscle
Not used much
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113
Q

Metyrosine

A

blocks tyrosine hydroxylase, ↓synthesis of catecholamines; pre-surgical tx of pheochromocytoma

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114
Q

Serotonin

A

decrease=depression, anxiety; excess = sleep; raphe nuc to limbic

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115
Q

GABA

A

major inhibitory in CNS, interneurons; ↑=anxiety relief; ↓ = seizures (↑NMDA activity)
GABAA - ↑Cl conductance (Barbs, Benzos, EtOH)
GABAB - ↑K, ↓Ca conductance (Baclofen)

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116
Q

Glutamate

A

major excitatory in CNS; inotropic, metabotropic; etoh blocks @ NMDA; NMDA receptor(glycine must bind) – learning, memory, long
term potentiation; ↑Glutamate = seizures

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117
Q

Glycine

A

inhibitory; brain stem & spinal cord interneurons; blocked by strychnine

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118
Q

Neuropeptides

A

endogenous opiates; endorphins, enkephalin, substance P

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119
Q

Cannabinoids

A

THC; memory, cognition, pain

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120
Q

What causes Parkinson’s?

A

Nigrostriatal dopaminergic neurons - SN to caudate/putamen (part of striatum); degeneration → ↓DA (& relative ↑Ach activity) → Parkinson’s

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121
Q

DA metabolism

A

tyrosine → l-dopa (dopa decarboxylase) → dopamine (MAO-B & COMT) → HVA; DA doesn’t cross BBB, l-dopa does cross BBB

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122
Q

L-Dopa (Levodopa)

A

Parkinson’s drug
symptomatic relief only; greatly metabolized in GI and periphery →nausea and vomiting, vasodialte(↑ DA receptor axn)
DA doesn’t cross BBB, l-dopa does cross BBB

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123
Q

Carbidopa/Levodopa

A

Parkinson’s Drugs
carbidopa: inh dopa decarboxylase; carbidopa does not cross BBB; ↑ l-dopa entry into brain→↓ dose required; ↓peripheral effects; ↓effectiveness w/ time (3-4 years) due to continued loss of DA neurons;
SE: nausea, postural hypotension, psychosis***(tx w/ clozapine, aripiprazole), insomnia, dyskinesia; Rapid withdrawal = NMS; Intraxn: MAOI’s → hypertensive crisis; CI: psychosis, malignant melanoma

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124
Q

Selegiline

A

Parkinson’s Drug
inh MAO-B dopamine availability; ↓ROS, may slow disease progression; used w/ l-dopa/carbidopa; insomnia; CI: w/ meperidine

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125
Q

Bromocriptine

A

Parkinson’s Drug

direct DA receptor agonist→ effectiveness does not ↓ with time; SE: erythromelalgia – red, tender, swollen feet

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126
Q

Pramipexole, Ropinirole

A

Parkinson’s Drugs

DA receptor agonist; well tolerated, initial tx; ↓ restless legs SE: sudden sleep

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127
Q

Amantadine

A

Parkinson’s Drug

antiviral; may ↑ DA release; SE: psychosis, seizures, spotting of skin; reddish blue spots on body

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128
Q

Benztropine

A

Parkinson’s Drug

anti-muscarinic; restores DA-Ach balance; ↓ tremor, ↓ rigidity; little effect on bradykinesia

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129
Q

Tolcapone

A

Parkinson’s Drug

COMT Inhibitors – prevent L-dopa degradation, dopamine available; Not as good as Selegiline. SE: liver disease

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130
Q

What NT changes occur in Alzheimer’s?

A

Confusion, memory loss, personality changes → anxiety, difficulty recognizing family/friends → loss of speech, appetite, bladder control
Degeneration of cholinergic neurons – nuc basalis of Meynert to cerebral cortex & hippocampus; ↓Ach levels; eventual ↓ in NE & 5HT

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131
Q

Memantine

A

Alzheimer drug
NMDA antagonist – prevents glutamate neurotoxicity→ may slow disease progression; SE: dizziness, confusion, hallucinations, mostly urinary

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132
Q

Donepezil, Tacrine, Rivastigmine, Galantamine

A 
Alzheimer drugs
cross BBB (diff. from, eg, neostigmine), Inhibit AChE in the brain; GI SEs, nausea, dizziness(Tacrine Liver probs)
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133
Q

Barbiturate characteristics

A

Bind GABAA, enhance axn independent of GABA(prolongs opening of Cl- channel); hypnosis; Low safety margin; life threatening withdrawal; schedule II of III; synergy w/ EtOH; Cyp450 inducer
SE: CNS depression, mood distortion, ↓respiratory drive, ↓BP, ↓REM sleep; CI: porphyria
Tx of OD: diuresis/alkalinization of urine, don’t give stimulant; SUPRA-additive w/ other CNS depressants

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134
Q

Phenobarbital

A

Barbiturate

Long acting, anticonvulsant

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135
Q

Phenobarbital

A

Barbiturate

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136
Q

Thiopental

A

Barbiturate

Ultra short acting, anesthesia induction

137
Q

Secobarbitol

A

Barbiturate

138
Q

Benzodiazapines cahracteristics

A

Bind GABAA complex, enhance axn only when GABA is present → ceiling effect, relatively safe; liver met (no Cyp); synergy w/ EtOH;
Eff: anti-anxiety, sedation, muscle relax(diazepam), anticonvulsant, NO CNS Depression(Barbits)
SE: dizziness, drowsiness, sedation, memory loss; esp. in elderly
Tolerance: when used chronically, discontinuation → insomnia, anxiety, seizures
CI: pregnancy, children, sleep apnea, not great in elderly
Tx: anxiety except OCD(w/SSRIs), PTSD(anti-D), agoraphobia(w/SSRIs), children(anti-D)

139
Q

Diazepam (Valium)

A

Benzodiazepine

long T1/2; tx: status epilepticus, alcohol/barbs withdrawal, muscle spasm/relaxant

140
Q

Chlordiazepoxide

A

Benzodiazepine

long T1/2; tx: alcohol/barbs withdrawal(tapered)

141
Q

Lorazepam

A

Benzodiazepine

int T1/2(

142
Q

Clonazepam

A

Benzodiazepine

Tx Absence seizures

143
Q

Flurazepam

A

Benzodiazepine

Long T1/2 = 74hrs; hypnotic; SE “hang over”

144
Q

Alprazolam

A

Benzodiazepine

short T1/2; anxiety + depression

145
Q

Midazolam (Versed)

A

Benzodiazepine

very short T1/2; anterograde amnesia in surgery, IV

146
Q

Temazepam, Triazolam

A

Benzodiazepine

Short acting hypnotic (rebound insomnia)

147
Q

Oxazepam

A

Benzodiazepine

Short acting

148
Q

Flumazenil

A

Benzo antagonist, IV only, reverse effects of above and below; may cause seizures w/ chronic Benzo/Barbs/TCAs

149
Q

When are Benzos not used and what is used instead?

A

OCD (SSRI)
Panic (SSRI)
PTSD (antidepressant)
Anxiety in kids (antidepressant)

150
Q

Zolpidem, Zaleplon

A

Bind to BZ1 subtype of GABA, causes sleep, rapid short action
SE: “blackouts,” amnesia, rebound insomnia, sleep driving, eating,

151
Q

Eszopiclone

A

Similar to Zolpidem(longer), activates all BZ receptors

Anti-anxiety and sedative

152
Q

Ramelteon

A

Sedative

Melatonin receptor agonist, no dependence or rebound

153
Q

Buspirone

A

5HT1A partial agonist; tx: anxiety w/out causing sedation; 2 weeks for effect; very low addiction potential no GABA effect; little to no sedation; no interaction w/ EtOH, benzos; Intraxn: ↑BP with MAOI’s

154
Q

Ethanol

A

GABAA is down-regulated & NMDA is up regulated with chronic use; causes sedation but decrease quality of sleep; Zero Order – 10g metabolized/hr(means a 12oz beer takes one hour to metabolize); Vaso- D hypothermia, ↓ADH effect diuretic

155
Q

Disulfiram

A

Inh aldehyde dehydrogenase

156
Q

Naltrexone

A

Treatment for alcohol

Blks reward pathway(β-endorphins are blkd from working on opioid receptors)

157
Q

Acamprosate

A

Alcohol treatment

Analogue of GABA; restores normal balance of GABA and glutamate

158
Q

General MOA of CNS stimulants

A

↑DA (& NE) levels
Effects – Low dose: ↑BP, ↑alertness, ↓appetite, euphoria
Med dose: tremor, restlessness, ↑respiration
High dose: behavioral repetition, psychosis Physical dependence, abuse potential

159
Q

Methylphenidate (ritalin, Concerta)

A

CNS Stimulant

tx: ADHD, narcolepsy, obesity

160
Q

Amphetamine (Adderall)

A

CNS Stimulant

tx: ADHD, narcolepsy, obesity; causes NE release

161
Q

Atomoxetine (Strattera)

A

CNS Stimulant

SNRI, (-)NE reuptake; tx: ADHD ; no abuse potential

162
Q

Caffeine

A

CNS Stimulant
blocks adenosine receptors, (-)PDE→ ↑cAMP; Eff: ↑alertness, ↑ gastric acid, diuresis vaso-C cerebral BV’s→ headache relief; High dose: tachy,
hypertension, insomnia

163
Q

Cocaine as CNS stimulant

A

CNS stimulant

inhibits NE re-uptake

164
Q

Baclofen

A

Centrally acting muscle relaxant
Agonist at GABAB (inh Ca++ channels presynaptically and opens K+ postsynaptically hyperpolarizes and inh NT release; Can also inh substance P(relieving pain)

165
Q

Diazepam

A

Centrally acting muscle relaxant

Acts on GABAA in the spinal cord to decrease spasticity

166
Q

Cyclobenzaprine (Flexeril)

A

Centrally acting muscle relaxants

Tx acute muscle spasm

167
Q

Carisoprodol

A

Centrally acting muscle relaxants

Central sedative

168
Q

Tizanidine

A

Centrally acting muscle relaxants

Agonist at α2 presynaptically reducing spasm

169
Q

Dantrolene

A

Centrally acting muscle relaxants

Interferes w/ Ca++ release from SR; Tx malignant Hyperthermia

170
Q

Botulinum Toxin

A

Centrally acting muscle relaxants

171
Q

Physical dependance

A

abnormal behavior and physical symptoms occur with withdrawal(not indicate addiction)

172
Q

Psychological dependance

A

Dysphoria and intense craving following withdrawal.(drive to avoid discomfort)

173
Q

Cocaine as drug of abuse

A

inhibits DA and NE re-uptake; Local anesthetic, vaso-c, energy, euphoria, all sympathomimetic sxs; Paranoid Psychosis; Major Cardiac probs;
Taken IV/smoke(fast), nasal(long high), chewing (slight high); cocaine bugs, Slow recovery(1-2yrs); Intense psych dependence;
rapidBP↑=cerebral hemorrhage

174
Q

Methamphetamine as drug of abuse

A

Release NE and DA, euphoria, energy, decreased appetite, increased BP, Cardiac toxic, high abuse, psychosis with weight loss, slow recovery, death by seizures, organ damage, stroke, heart attack, Meth bugs, toxic with ETOH

175
Q

Nicotine as drug of abuse

A

Most addictive, increase 5HT and DA release, increase memory, learning, alertness; very reinforcing, inc BP and HR, mild stimulant

176
Q

Alcohol as drug of abuse

A

withdrawal worst, CNS depressant

Tx: naltrexone + Prozac

177
Q

Benzos and Barbiturates as drugs of abuse

A

Combined with other drugs but rarely abused; CNS depressant, flunitrazepam-Rape

178
Q

Opioids as drugs of abuse

A

Inc DA, euphoria, reduced anxiety, sedative, tolerance, abuse seen in health professionals, facilitate reward pathway

179
Q

Marijuana (THC)

A

Least addictive of drugs of abuse

mild euphoria, slows time, psych dependence, impairs short term memory, MEDS-anti-emetic, increase appetite, analgesia

180
Q

LSD drug of abuse

A

Euphoria, visual hallucinations, bind 5HT2, bad trips/flashbacks, “shrooms”

181
Q

Mescaline as drug of abuse

A

Similar to LSD but less potent

182
Q

MDMA (Ecstasy)

A

Inc 5HT release, inc HR and BP, hyperthermia and dehydration, memory problems

183
Q

Phencyclidine (PCP, angel dust)

A

NMDA receptor antagonist, analgesia (Ketamine is derivative), aggressive

184
Q

Ketamine

A

NMDA receptor antagonist; “date rape”, sense of floating

Dissociative analgesia

185
Q

TCA’s

A

Inh reuptake of 5HT & NE; also block M, α, and H receptors
SE: sedation (H block), memory loss (Ach block), analgesia (↑NE), cardiotoxicity (Torsades), ↓seizure threshold convulsions, coma, α1 block – postural hypotension, reflex tachy, dry mouth; weight gain?, SIADH, sexual dysfunction, suicidal tendencies Drug Intraxn: MAOI’s → serotonin syndrome – hyperpyrexia, seizures, coma; wait 2-3 weeks after MAOI; SSRI’s - ↑TCA levels, toxicity; Amphetamine – hypertension; Cocaine – arrhythmias
Tx: depression, panic attacks, chronic pain, fibromyalgia, neuropathic pain(most common use), enuresis

186
Q

Amitriptyline, Imipramine

A

TCA Antidepressant

tertiary amine; more sedating; → active metabolite (Imipramine – tx enuresis)

187
Q

Nortriptyline, Desipramine

A

TCA Antidepressant

secondary amine; less sedating; active form, less anti-ACh effects that tertiary

188
Q

MAOI’s

A

Antidepressant
MAO-A breaks down 5HT and NE and tyramine
MAO-B breaks down DA
Tx: depression
SE: Hypertensive crisis with tyramine ingestion(in foods), also block α and m(same side effects as above)

189
Q

Phenelzine (Nardil)

A

MAOI

Antidepressant

190
Q

Clomipranine

A

TCA used only for OCD, works like an SSRI

191
Q

SSRI’s

A

Inh 5HT reuptake; take 2-3 weeks for effect; mild SE’s
SE: GI upset, weight loss, CNS stimulation – anxiety, insomnia; sexual dysfunction, SIADH is possible, no ANS effects
Drug Intraxn: MAOI’s/St John’s Wart – serotonin syndrome; TCA’s - ↑TCA levels, toxicity; Opioids (w/ fluoxetine) - ↓ opioid effect
Tx: DOC depression, panic, OCD; agoraphobia, bulimia, alcoholism, kids

192
Q

Fluoxetine (Prozac)

A

SSRI for depression

very long T1/2, 5 weeks(and metabolite) to clear; inh Cyp2D6 (↓effect of codeine, hydrocodone, oxycodone), insomnia

193
Q

Paroxetine (Paxil)

A

SSRI

OCD, agoraphobia SE: sedation, inh cyp2D6; CI: Pregnant

194
Q

Sertraline (Zoloft)

A

SSRI

Safer than Fluoxetine w/ shorter duration of action

195
Q

Citalopram (Celexa)

A 
SSRI
faster onset (1-2 weeks)
196
Q

Escitalopram (Lexapro)

A

SSRI

Faster onset than citalopram

197
Q

Venlafaxine (Effexor)

Desvenlafaxine (Pritiq)

A

SNRI

Inh 5HT & NE reuptake; tx: depression, more for chronic pain; more SE’s than SSRIs less than TCAs, ↑BP

198
Q

Duloxetine (Cymbalta)

A

SNRI

5HT & NE reuptake, greater NE effect; tx: depression, neuropathic pain, hepatotoxic

199
Q

Bupropion (Wellbutrin)

A

Antidepressant in other category
Inh Dopamine reuptake; tx: depression, ADHD, smoking cessation; less sexual dysfunction; can cause seizures, anxiety and insomnia at high doses, wt loss CI: pts w/ seizures or head trauma

200
Q

Mirtazapine (Remeron)

A

Antidepressant in other category
blocks α2→↑5HT & NE but blocks 5HT2A, 3 receptors→ fewer SSRI SE’s (less sexual dysfunction); tx: depression w/ insomnia; SE: sedation, appetite, weight gain, dry mouth

201
Q

Atomoxetine (Strattera)

A

Selective NE reuptake inh. Tx of ADHD

202
Q

Trazodone (Desyrel)

A

partial agonist at 5HT1A & blocks 5HT2; tx: sleep aid, pain; SE: sedation, priapism

203
Q

St. John’s Wart

A

may block 5HT & NE reuptake; SE: metabolism of other drugs(anything w/ a small therapy range; careful), especially protease inhibitors

204
Q

Schizophrenia

A

hallucinations, lack of affect, apathy, delusions;↑dopaminergic activity

205
Q

Dopaminergic systems in brain

A

Nigrostriatal - SN to caudate/putamen (part of striatum); posture & movement; ↓ in activity → extrapyramidal symptoms (Parkinson’s)
Mesolimbic-Mesocortical – ventral tegmental area (midbrain) to limbic-nucleus accumbens (striatum)/frontal cortex; reward, emotions, cognition; ↑ activity → psychosis
Pituitary – Arcuate nuc (hypothalamus) to ant pituitary; inh prolactin secretion

D2 block for tx of “positive” symptoms - delusions
D4 & 5HT2A block for tx of “negative” symptoms – apathy

206
Q

Typical antipsychotics

A

Most block D2, α, Muscarinic, and Histamine receptors
Effect: ↓ fear, ↓hallucinations, ↓anxiety, antiemetic
Extrapyramidal symptoms (EP’s) – akathisia, dystonia, tremor, tardive dyskinesia: tx by bringing dopamine and Ach activity into balance; so drugs with more anti-Ach have ↓EP symptoms

207
Q

Tardive dyskinesia with antipsychotics

A

stereotypic oral facial movements probably due to dopamine receptor sensitation, after long term use

208
Q

Common SE of antipsychotics

A

Other SE: Postural hypotension, dry mouth blurred vision, inhibition of ejaculation, sedation and weight gain(a lot), Neuroleptic syndrome(rare, tx: dantrolene), hyperprolactinemia, anti-m effects: dry mouth, constipation, hypotension, sedation

209
Q

Thioridazine (Mellaril)

A

Phenothiazine antipsychotic blocks D2

Low potency less EPS symptoms, retinal deposits

210
Q

Fluphenazine (Prolixin)

A

Phenothiazine antipsychotic blocks D2

High potency EPS symptoms

211
Q

Trifluoperazine

A

Phenothiazine antipsychotic blocks D2

High potency EPS symptoms

212
Q

Chlorpromazine (Thorazine)

A

Phenothiazine antipsychotic blocks D2

Low potency less EPS symptoms, corneal deposits, jaundice, tx N/V

213
Q

Haloperidol (Haldol)

A

Conventional antipsychotic specific for D2
High potency causes worst EPS Sx of antipsychotics, no ACh effects, DOC – acute highly sedating
We can see here from the drug haloperidol that it is the block of the D2 receptors that are responsible for the EP symptoms.
Remember that you want to block the D2 receptors in the case of psychosis because too much DA will cause this problem. The goal of Tx is to bring the DA and ACh back into their proper ratios.

214
Q

New generation/atypical antipsychotics

A

Block 5-HT2a, D4/D2, α, and H1 receptors

Less EPS and anticholinergic effects, treat both positive and negative symptoms, all have wt gain (except aripiprazole)

215
Q

Olanzapine (Zyprexa)

A

Atypical Antipsychotic

Blks D4 Also used in OCD, anxiety, depression, Tourette’s SE: Weight gain, hyperglycemia(worst), Type II diabetes

216
Q

Clozapine (Clozaril)

A

Atypical Antipsychotic

Blks D4, no tardive or EPS, agranulocytosis

217
Q

Quetiapine (Seroquel)

A

Atypical Antipsychotic

No prolactin increase, SE: sedation, adjunct in depression tx

218
Q

Risperidone (Risperdal)

A

Atypical Antipsychotic

Lengthens QT interval (no use in elderly)

219
Q

Ziprasidone (Geodon)

A

Atypical Antipsychotic

Lengthens QT interval (no use in elderly)

220
Q

Aripiprazole (Abilify)

A

Atypical Antipsychotic
blocks 5HT2A; partial agonist at D2 & 5HT1A; “dopamine stabilizer”; anti- anxiety, blk – and + Sxs;↓EP’s, ↓prolactin effects; SE: orthostatic hypotension, hyperglycemia, sedation, seizures, ↓esophageal motility

221
Q

Lithium (Eskalith)

A

Mood stabilizer Tx for bipolar
kidney excretion, competes w/ Na for resorption; Thiazides, NSAID’s, & ↓Na→↑ [Li]; SE: nausea, headache, tremor, ↓thyroid function, edema, weight gain, diabetes insipidus (tx w/ amiloride); narrow therapeutic range; Toxicity: nausea, tremor, fasciculations →confusion, ataxia, seizures, arrhythmias, coma

222
Q 
Valproic acid (Depakene)
Divalproex (Depakote)
A

anticonvulsant and mood stabilizer; rapid onset blocks Na channels, increase GABA; monitor liver enzymes

223
Q

Carbamazepine (Tegretol)

A

anticonvulsant and mood stabilizer, increase Na channel inactivation

224
Q

Topiramate (Topamax)

A

anticonvulsant and mood stabilizer, blocks Na channels, increase GABA

225
Q

Lamotrigine (Lamictal)

A

anticonvulsant and mood stabilizer, Block voltage gated Na channels

226
Q

Gapapentin (Neurontin)

A

Mood stabilizer

Tx pain; CI: pregnancy (not good for bipolar disorder)

227
Q

Partial seizure

A

Partial: Simple – jerking, ~20 sec, preservation of consciousness

228
Q

Complex seizure

A

impaired consciousness

229
Q

Generalized seizure

A

Tonic-Clonic (Grand Mal) – loss of consciousness, muscle contractions

230
Q

Absence (Petit Mal) seizure

A

staring, ~30 sec (low threshold Ca++ in Thalamus)

231
Q

Possible cause of seizures and treatment strategy

A

Possible due to ↓GABA or ↑Glutamate (NMDA) activity – (tx: blk Na+ Channels and enhance GABA)
Most anticonvulsants are CI: pregnancy (most are teratogens)

232
Q

Phenytoin (Dilantin)

A

Anticonvulsant
prolongs Na channel inactivation; Tx: partial & tonic-clonic seizures; Induces P450, ↑ [warfarin], ↑oral contraceptive metabolism, dose dependent elimination; SE: gingival hyperplasia, hirsutism, nystagmus, double vision

233
Q

Carbamazepine (Tegretol)

A

Anticonvulsant
blocks Na channels; Tx: partial(DOC) & tonic-clonic seizures, trigeminal neuralgia, bipolar disorder; Drug intraxns, induces P450, SE: blood dyscrasias(anemia, agranulocytosis), GI upset;

234
Q

Phenobarbitol (Luminal)

A

Anticonvulsant

prolongs Cl- opening at GABA; Barbiturate; Tx: partial & tonic-clonic

235
Q

Gapapentin (Neurontin)

A

Anticonvulsant
GABA analog but nebulous mech; Tx: adjunct for partial & tonic- clonic seizures, neuropathic pain, bipolar disorder; kidney excretion

236
Q

Pregabalin (Lyrica)

A

tx: neuropathic pain, fibromyalgia

237
Q

Topiramate (Topamax)

A

Anticonvulsant

blocks Na, ↑GABA, ↓glutamate(less teratogenic)

238
Q

Ethosuximab (Zarontin)

A

Anticonvulsant

↓Ca current in thalamus; Tx: absence seizures(DOC); SE: GI pain

239
Q

Valproic Acid (Depakene)

A

Anticonvulsant
↓repetitive firing; Tx: absence + tonic-clonic(DOC), myoclonic, bipolar, migraine; SE: hepatotoxicity; Many drug intraxns

240
Q

Clonazepam (Klonopin)

A

Benzo used for status epilepticus

241
Q

Diazepam (Valium)

A

Benzo used for status epilepticus

242
Q

Lorazepam (Ativan)

A

Benzo used for status epilepticus

243
Q

Stevens-Johnson Syndrome and erythema multiform

A

Hypersensitivity autoimmune (immune complex) reaction; can happen w/ anticonvulsants; Epidermis separates from dermis; Tx: discontinue drug
Erythema multiforme, arthritis, nephritis, CNS abnormalities, myocarditis
DRUGS : Phenytoin, Carbamazepine, Oxcarbazapine, Phenobarbital, primordine, Lamtrigine, Tiagabine, Ethosuximide, Valproic Acid

244
Q

Digitalis (foxglove, Digitalis purpurea, draft evaders, arrow poison)

A

Positive Inotropic agent
Inh Na/K-ATPase → ↑ IC Na (↓ IC K) → ↓ Ca expulsion so ↑ IC Ca → ↑ contractility, ↓ HR, ↑ CO & vaso-D in failing hearts only, ↓ AV conduction; Tx: CHF, A-fib, A-flutter
SE: GI upset → lower dose, cardiac (brady, AV block, bigeminy) → cease therapy; CNSToxicity: ↑ by Ca, ↓ by K; Tx toxicity w/ K or DigiBind for ODCI(relative): quinidine (↑ serum drug), K losing drugs, ß-blockers, cardioversion (except v-fib); T1/2= 40hrs(1wk until steady state)

245
Q

Loop diuretics

A

Furosemide, torsemide, bumetanide, ethacrynic acid

All sulfa drugs except for Ethacrynic acid which is most ototoxic

246
Q

Acetazolamide (Diamox)

A

Carbonic Anhydrase inhibitor diuretic

Oral tx for Acute Moutain sickness

247
Q

Methazolamide (Neptazane)

A

Carbonic Anhydrase inhibitor diuretic

248
Q

Brinzolamide (Azopt)

A

Carbonic Anhydrase inhibitor topical for glaucoma

249
Q

Dorzolamide (Truspot)

A

Carbonic Anhydrase inhibitor topical for glaucoma

250
Q

Thiazide + other diuretics

A

Indapamide, Metolazone, Hydrochlorothiazide

251
Q

K-sparing diuretics

A

Inh Na/K exchange (collecting ducts) → ↑Na excretion, K sparing Hyper-K, acute renal failure Tx: CHF, combined with K losing drugs, cirrhosis
CI: Hyper-K
Triamterene, Amiloride (DOC for lithium induced DI), Spironolactone, Eplerenone

252
Q

Aldosterone antagonists

A

Diuretics

inh. Aldosterone receptors in distal/collecting duct; Tx: edema assoc w/CHF, cirrhosis, nephrotic syndrome
- Spironolactone – ↑ survival in CHF, most effective in hyperaldosteronism; SE: gynecomastia
- Eplerenone – ↑ survival in CHF, ↓ endocrine SE’s, CYP3A4 met

253
Q

B type natriuretic peptide

A

Nesiritide (Natrecor) – Tx: acute decompensated CHF; will ↓PCWP

254
Q

Carbonic anhydrase inhibitor action for Diuresis

A 
Inh CA (proximal tubule) → ↓ bicarb reabsorption, ↑ Na excretion due to lack of H+ in lumen ↑ K exc. in DCT and collecting duct. Tx: met alkalosis, acute mtn sickness, glaucoma, alkalinize urine CI: cirrhosis, sulfonamide hypersensitivity; Tox: renal sotnes, renal K+ wasting, hyperchloremic metabolic acidosis
Effective for only a few days
255
Q

Loop diuretic MOA

high Na+ excretion

A

Blk Na-K-2Cl cotransport (thick asc. loop)→ ↑Na, K, Mg, Ca, H+ excretion Reducing concentration gradient in the renal medulla imparing concentration and diluting capacity of kidney.
SE: OH DANG! – Ototoxicity, Hypokalemia, Dehydration, Allergy(sulfa), Nephritis(interstitial), Gout
Tx: CHF, pulm edema, acute renal failure, hyper-K, hyper-Ca, CI: avoid NSAIDs

256
Q

Thiazide diuretics MOA

A

Inh Na/Cl reabsorption (distal diluting site) → ↑Na, K, Cl excretion; ↑Ca++ reabsorption; Tx: HTN, CHF, nephrolithiasis, Nephrogenic DI Tox: Hypo-K, met alkalosis, Ca sparing (↓ stones), hyperglycemia(may ↓ release of insulin- Type II DM), hyperlipidemia, hyperuricemia, liver metabolism, Sulfa allergy

257
Q

Osmotic Diuretics

A

Increased osmotic activity, water retention (prox, loop, CD) (freely filterable agents)
Dehydration, hyper-Na
CI: severe CHF (early over-expansion of intravascular space)
Mannitol

258
Q

Desmopressin

A

ADH agonist, strong V2 agonist, increases factor VIII and vWF

259
Q

Vasopressin

A

ADH agonist

260
Q

Demeclocycline

A

ADH antagonist, produces nephrogenic DI, SE: hyponatremia

261
Q

Lithium and diuresis

A

ADH antagonist, produces nephrogenic DI, SE: hyponatremia

262
Q

Conivaptan, Tolvaptan

A

V1 and V2 vasopression receptor antagonists; ↑urine output

263
Q

Methyclothiazide (Enduron)

A

Thiazide diuretic

264
Q

HMG-CoA reductase Inh “statins”

A

Lovastatin – blk rate limiting step in cholesterol synthesis; most effective in heterozygous familial hypercholesterolemia or combined hyperlipoproteinemia; CI: pregnancy

265
Q

Pravastatin (Pravachol)

A

HMG-CoA reductase Inh

266
Q

Simvastatin (Zocor)

A

HMG-CoA reductase Inh

267
Q

Fluvastatin (Lescol)

A

HMG-CoA reductase Inh

268
Q

Atorvastatin (Lipitor)

A

HMG-CoA reductase Inh

269
Q

Rosuvastatin (Crestor)

A

HMG-CoA reductase Inh

270
Q

Pitavastatin (Livalo)

A

HMG-CoA reductase Inh

271
Q

Cholestyramine (Questran)

A

Bile acid binding resin; inh reabsorption of bile acids from the gut ↑LDL receptor expression in the liver; NOT effective in homozygous familial hyperlipidemia(no LDL receptors); SE: tastes horrible, GI-constipation and bloating, ↓ absorption of fat-soluble vitamins and Cholesterol gallstones; Impair absorption of digitalis, thiazides, tetracycline, thyroxine or ASA
Similar: Colestipol (Colestid), Colesevelam (WelChol)

272
Q

Nicotinic Acid (Niacin)

A

Inh the secretion of VLDL from the liver, ↑HDL; Most effective in heterozygous familial hypercholesterolemia(combo wil bile-acid binding resins), also in familial combined hyperlipoproteinemia, familial dysbetalipoproteinemia, hypercholesterolemia

273
Q

“Fibrates” -Gemfibrozil -Fenofibrate

A

Ligand for PPAR-α: Stimulate Lipoprotein lipase to increase hydrolysis of VLDL; SE: Myositis, hepatotoxicity, cholesterol gallstones
Effective in: familial dysbetalipoproteinemia and hyperTG NOT effective: primary chylomicronemia and familial hypercholesterolemia

274
Q

Ezetimibe (Zetia)

A

Inh the absorption of dietary and biliary cholesterol from the intestine.

275
Q

Orlistat (Xenical)

A

Wt loss; inh pancreatic lipase; SE: oily stool

276
Q

Alirocumab, Evolocumab

A

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors used for high cholesterol/lipid

277
Q

What are the general treatment modalities for angina?

A

Nitrates/Nitrites for vasodilation
Ca channel blockers for vasodilation, decrease HR
Beta Blockers to reduce O2 demand on heart
Phosphodiesterase-5 inhibitors to vasodilate

278
Q

Nitrates and Nitrites for angina

A

Nitrates and Nitrites – sublingual
Most effect on veins(↓preload) also redistributes coronary blood flow; nitrite ion →NO →↑cGMP →vaso-D; Tx: angina, CN poisoning(Sodium Nitrite forms methemoglobin) Tolerance develops quickly, Monday disease in explosive manufacturers
-Nitroglycerin, Isosorbide dinitrate, Amyl nitrite (inhaled, euphoria)

279
Q

Calcium channel blockers for angina

A

Calcium Channel Blockers – oral; mainly renal excretion
-Verapamil–strongest cardiac effects; ↓HR, (-)inotrope, depress SA/AV; SE:constipation, depress cardiac too much AV block and cardiac arrest, inh platelets and insulin secretion -Diltiazem (Cardizem) – in between Verapamil and Nifedipine; depress SA/AV node directly Dihydropyridines- “-dipines”
Strongest vasodilators-arterioles; reflex tachycardia
-Nifedipine (Procardia) – oral/topical; Amlodipine (Norvasc), Isradipine

280
Q

Beta blockers for angina

A

Beta Blockers
↓cardiac workload →↓O2 demand; ↓HR →↑perfusion time; ↓vaso-C
-Propranolol (ß),Metoprolol(ß-1), Atenolol(ß-1)

281
Q

PDE-5 Inhibitors for angina

A 
Phosphodiesterase-5 Inhibitors - oral
Inh PDE5(& some PDE6) →↑cGMP; Tx: erectile dysfunction; SE: headache, flushing; CI: Nitrates -Sildenafil (Viagra) – ~60 min to axn; CYP3A4; CI: nitrates, α blockers; SE: visual
-Vardenafil (Levitra) – more selective for PDE5→↓visual SE; faster onset of axn
-Tadalafil (Cialis) – longest duration of axn; allows for crazy weekends in Vegas
282
Q

Nitroglycerin

A

Nitrate/nitrite used for angina

283
Q

Isosorbide dinitrate (Isordil)

A

Nitrate/nitrite used for angina

284
Q

Isosorbide mononitrate (Ismo)

A

Nitrate/nitrite used for angina

285
Q

Nifedipine (Procardia)

A

Dihydropyridine type Ca channel blocker used for angina

286
Q

Sildenafil (Viagra)

A

PDE5 inhibitor
Used for angina (and other uses)
~60 min to axn; CYP3A4; CI: nitrates, α blockers; SE: visual

287
Q

Vardenafil (Levitra)

A

PDE5 inhibitor
Used for angina (and other uses)
more selective for PDE5→↓visual SE; faster onset of axn

288
Q

Tadalafil (Cialis)

A

PDE5 inhibitor
Used for angina (and other uses)
longest duration of axn; allows for crazy weekends in Vegas

289
Q

Avanafil (Stendra)

A

PDE5 inhibitor

Used for angina (and other uses)

290
Q

Ranolazine (Ranexa)

A

Treatment for angina

oral; Inh. PFox, inh. Late Na current; ↓LV wall stiffness; Tx: chronic stable (not 1st line); SE: CYP3A4, teratogenic

291
Q

Bosentan

A

Treatment for angina

oral; endothelin receptor antagonist; only use in severe pulmonary HTN

292
Q

Erythromycin

A

Macrolide–liver elim., good for kideny failure, not good for UTI’s, protein synth inhibitor
reversibly binds 50S – inh translocation steps; alternative for penicillin allergy and when kidney failure; SAFE; spectrum similar to Pen G (gram +; (-) is resistant); Tx erysipelas due to GAS, pneumonia due to M. pneumoniae, chlamydia, and Legionnaire’s disease, also for Syphilis(those allergic to Pen G), can penetrate prostatic fluid; acid-sensitive – must be enteric-coated; inh. CYP3A4; antagonism w/ chloramphenicol(same binding site); no CNS; SE: GI disturbances, DIARRHEA, elevated hepatic enzymes, cholestatic jaundice, ototoxicity, may prolong QT, torsades; Resistance: is due to a Methylase(modify binding site); active pump or esterases & 50S mutation

293
Q

Clarithromycin (Biaxin)

A

Macrolide–liver elim., good for kideny failure, not good for UTI’s, protein synth inhibitor
similar mechanism; penetrates lung and macrophages: tx MAC(in immunocompromised), H. pylori-associated duodenal ulcers, community-acquired pneumonia (CAP)

294
Q

Azithromycin (Zithromax)

A

Macrolide–liver elim., good for kideny failure, not good for UTI’s, protein synth inhibitor
similar mechanism; dosed once daily; DOC for Legionnaires; effective against chlamydia and gonorrhea(ceftriaxone is DOC), pediatric otitis media, pharyngitis, and MAC prophylaxis; less effect on CYP3A4(NOT metabolized by P450 system; but still excreted in bile) and fewest overall SE/interactions

295
Q

Telithromycin (Ketek)

A

Ketolides (altered Macrolide for the resistant organisms)
- Telithromycin(oral) – binds 50S; broad spectrum; tx respiratory pathogens, intracellular and atypical bacteria(for erythro/PCN resistant); SE serious hepatotoxicity

296
Q

Clindamycin (Cleocin)

A

Protein synth inhibitor
(oral)binds to 50S; primarily in Tx of anaerobic bacteria infections – Bacteroides fragilis; effective w/ pyrimethamine(inh DHF reductase) in tx toxoplasmic encephalitis in patients w/ AIDS, Tx Osteomyelitis(b/c Staph causes it); SE well known cause of pseudomembranous colitis

297
Q

Dalfopristin; Quinupristin (Synercid)

A

Streptogramins
(IV)– irreversibly blocks ribosome function 50S; tx vancomycin-resistant Enterococcus faecium –not faecalis (VRE); inh. CYP3A4; CI: breast-feeding, kids, prego’s, etc

298
Q

Linezolid (Zyvox)

A

Oxazolidinone
reversible, non-selective inhibitor of MAO; blks formation of 70s – binding 50s; effective only against aerobic gram +; bacteriostatic; oral bioavailability 100%; metabolized via non- enzymatic oxidation (no interactions); tx VRE, MRSA, bacterial pneumonia; SE superinfection CI: hypersensitivity, pheochromocytoma

299
Q

Aminoglycosides

A

Protein synth inhibitor
they bind irreversibly 30S and inhibiting initiation complex, blocking translation, and incorporating the wrong AA – Require Oxygen dependent active transport. Concentration dependent killing – Bactericidal(time dependent w/ PAE = 1 time daily); horrible oral absorption and CSF penetration; inh. gram – bacilli (AEROBIC coverage only); effective particularly against Pseudomonas aeruginosa; also indicated if suspicion of sepsis; SE ototoxicity, nephrotoxicity, NMJ inhibition (serious toxicity – tx w/ Ca++ gluconate or neostigmine); Used ONLY to tx severe systemic infections; renal excretion

300
Q

Gentamicin

A

Aminoglycoside
(IV) topical application for tx burns and wounds; bactericidal in vitro against 95% S. aureus; DOC tularemia, w/ penicillin to tx Pseudomonas; (monitor plasma levels)

301
Q

Tobramycin

A

Aminoglycoside

IV) tx of severe infections (monitor plasma levels

302
Q

Amikacin (Amikin)

A

Aminoglycoside

IV) gentamycin-resistant infections may respond to this instead (monitor plasma levels

303
Q

Streptomycin

A

Aminoglycoside
(IV) tx tularemia, bubonic plague (w/ doxycycline), Brucella, TB (second line), endocarditis(in combo – due to staph, strep, or enterococcus)

304
Q

Spectinomycin

A

Aminoglycoside

(off market) – tx uncomplicated gonorrhea in patients who are allergic to ceftriaxone,

305
Q

Neomycin

A

Aminoglycoside
(topical); tx hepatic encephalopathy(NH4+ due to GI bacteria); prep for colon surgery- suppresses aerobic flora SE: severe hepatotoxicity if injected, contact dermititis

306
Q

Paromomycin

A

Aminoglycoside

(IV) tx intestinal amebiasis, Cryptosporidium parvum infections

307
Q

Chloramphenicol

A

reversibly binds 50S (anaerobes); bacteriostatic; oral; 100% oral absorption, CNS penetration; not effective against E. histolytic or pseudomonas; resistance due to bacterial acetyl transferase; distributed widely (including CNS & eyes); second line Tx typhoid fever (bactrim first), meningitis(very effective; DOC is PCN), Rickettsia/brucellosis/RMSF(DOC is Doxycycline), topical tx eye infections, Infections from Gram(-) organisms; inh CYP450 - ↑ effect warfarin/phenobarbital/phenytoin, ↓ effect penicillin – metabolized in liver(90%) conjugated with glucoronic acid; SE: gray baby syndrome(inh mito.), deadly aplastic anemia(genetic) and bone marrow depression(does dependent-reversible – by binding the mitochondria 70S ribosomes)

308
Q

Tetracyclines general

A

(oral) G(+ &-) and many of the big tough micro boys; tx H. pylori w/ metronidazole + bismuth; tx M. pneumonia, chlamydia, Lyme Disease(also ampicillin), Vibrio cholera, plague (w/ streptomycin), Brucella (w/ aminoglycoside), RMSF; bind specifically to 30S – blking access of the amino acyl-tRNA to the mRNA-ribosome complex; bacteriostatic; distribution wide except CNS and joints; aluminum and calcium salts may greatly inhibit intestinal absorption; SE: deposits in bone and teeth(like to go where Ca+ is), overgrowth of resistant flora(candida – like the inhaled corticosteroids); CI: pregnancy and children

309
Q

Tetracycline

A

Broad spectrum inhibitor of protein synthesis

short acting SE: skin eruption w/ sunlight

310
Q

Demeclocycline

A

Tetracycline

intermediate acting; SE: inh. ADH and skin eruption after sunlight

311
Q

Doxycycline

A

Tetracycline

(oral, IV) long acting – less intraxn w/ cations SE: skin eruption w/ sunlight

312
Q

Minocycline

A

Tetracycline

(oral, IV) long acting; ototoxicity – less intraxn w/ cations; 100% absorption on empty stomach

313
Q

Tigecycline

A

Glycylcycline
(IV) derivative of minocycline; binds 30S; bacteriostatic; Tx: MRSA, MRSE, PRSP, VRE; biliary excretion; SE: same as tetracyclines

314
Q

Nitrofurantoin (Furadantin)

A

UTI drug
broad spectrum; Good for E. coli, S. pyogenes, Citrobacter, Klebsiella, enterobacter; no proteus and pseudomonas coverage; > effect in acidic urine; SE: brown urine, methemoglobinemia, hemolysis, interstitial pulmonary fibrosis, severe polyneuropathies

315
Q

Methenamine Mandelate (Mandelamine)

A

UTI Drug
decomposes to formaldehyde in the urine and binds amino groups; bactericidal; mandelate acidifies urine; mainly effective against E. coli; resistance does not develop; non-toxic

316
Q

TMP-SMX for UTI

A

SE: thrombocytopenia due to folate metabolism interference; DOC for UTI’s

317
Q

Treatments for UTI

A

Nitrofurantoin, methenamine mandelate, nalidixic acid, TMPSMX,, cephalosporines, gentamicin, tobramycin, amikacin, ampicillin, amoxicillin, some fluoroquinolones

318
Q

DOC for listeria

A

Ampicillin

319
Q

Fluoroquinolone MOA

A

enter thru porin channels, inh. DNA gyrase!(topoisomerase II – which inh the resealing of nicked DNA = cleavage of DNA(Gram -); and topoisomerase IV – needed for cell division(Gram +);bactericidal

320
Q

Ciprofolxacin

A

2nd Gen. Fluoroquinolone
oral; broad spectrum bactericidal; highly active in vitro, especially against Pseudomonas aeruginosa and MRSA; less effective against gram +, anaerobes, and horrible CNS penetration, poor Strep pneumo coverage; DOC prophylaxis of inhalational anthrax; tx Shigella, soft tissue infections; SE: transient ↑ LFTs, tendon rupture, and QT prolongation, seizures in other fluoroquinolones and not cipro.

321
Q

Norfloxacin

A

1st Gen. Fluoroquinolone

322
Q

Ofloxacin

A

2nd Gen. Fluoroquinolone

323
Q

Moxifloxacin (Avelox)

A 
3rd Gen. Fluoroquinolone
IDEAL - oral once-a-day; broad spectrum; better activity against penicillin- susceptible and –resistant pneumococci (Strep pneumo) (better gram +), better anaerobic coverage, better CNS penetration; tx CAP; SE: should be avoided in patients with long QT/patients receiving class IA (quinidine, procainamide, disopyramide) or III antiarrhythmics (amiodarone, sotalol, etc.)
324
Q

Gatifloxacin (Zymar)

A

3rd Gen. Fluoroquinolone

topical for eye infections; off the market in 2006 due to SE: five-assed monkey

325
Q

Metronidazole

A

DOC E. histolytica, G. lamblia, T. vaginalis, also for tx B. fragilis, C. difficile, & Gardnerella; SE: GI irritation, metallic taste, disulfiram-like(avoid EtOH), red urine

326
Q

What are the first line TB drugs?

A

Isoniazid, Rifampin, Ethambutol, Pyrzinamide

Rifabutin, Streptomycin

327
Q

What are the second line TB drugs?

A

Aminosalicylic acid, Ethionamide, Rifapentine, Capreomycin, Clofazimine, Ciprofloxacin, Levofloxacin, Ofloxacin, Kanamycin

328
Q

Isoniazid

A

TB drug 1st line
(oral)#1 stunna prophylaxis; oral; inh mycolic acid(gets intracellular) –bactericidal in rapidly dividing organisms; always given in combo w/ at least one other antiTB drug; rapid(inuits, Natives Amer) vs slow(blacks/whites) metabolizers; SE: CNS stimulation, peripheral neuropathy(due to B6 def), liver damage, hemolysis (G6PD deficiency) – INH and Rifampin given together

329
Q

Ethambutol

A

TB drug 1st line
nh arabinosyl transferase; bacteriostatic; given w/ at least one other antiTB drug; renal excretion; good for MDR TB; SE: optic neuritis (decrease of visual acuityand loss of red-green perception)– not used in kids –last resort(given w/ vision tests; reversible if early detection)

330
Q

Rifampin

A 
TB drug 1st line
broad spectrum(G + and -) and all mycobaterium; inh. DNA-dependent RNA polymerase; bactericidal; activity approaches that of INH; effective against leprosy; SE: orange secretions(urine, sweat, tears), induces p450(not in HIV+ pts – switch w/ Rifabutin), decreases effectivenss of birth control
331
Q

Pyrazinamide

A

TB drug 1st line

bactericidal; SE: hepatic injury

332
Q

Streptomycin and TB

A

2nd line TB drug

ront-line durg, but may be dropped down to second line; can’t affect intracellularly

333
Q

Ethionamide

A

2nd line TB drug

oral) neurotoxic(peripheral neuropathies – B6 def

334
Q

Capreomycin

A

2nd line TB drug

(IM) nephrotoxic and ototoxicity

335
Q

Rifabutin

A

2nd line TB drug
(oral) front line in HIV+; taking protesase inh (can by prophylaxis in AIDS pt); less inducer of P450 ; urine discoloration, thrombocytopenia, polymyalgia

336
Q

Drugs used in leprosy

A

Triple drug regimen for 6-24 months
Dapsone
Rifampin
Clofazamine

337
Q

Dapsone

A

(oral) DOC leprosy and for P. jiroveci– start w/ low dose and increase over time; PABA antagonist; SE: methemoglobinemia, hemolysis(in G6PD def pt), peripheral neuropathy, nasal obstruction(will resolve) and cause erythema nodosum leprosum(ENL)

338
Q

Clofazamine

A

Treatment for leprosy
binds preferentially to mycobacterial DNA(high GC content in mycobacterium); SE: crystalline deposits(red-brown skin discolor), hepatotoxic (No ENL)

339
Q

Thalidomide

A

DOC erythema nodosum leprosum, tx HIV wasting syndrome; reduces levels of TNF-α; oral; pregnancy Category X

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