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Pharmacology Flashcards

1
Q

vitamin D analogs

A

e.g. calcipotriene (calcipotriol), calcitriol, tacalcitol

bind and activate vitamin D receptor (a nuclear TF) –> inhibition of keratinocyte proliferation, stimulation of keratinocyte differentiation, inhibits TC proliferation and other inflammatory mediators

bottom line: anti-inflammatory that is used to tx things like psoriasis

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2
Q

cyclosporine

A

inhibits NFAT (nuclear factor of activated TCs) –> impairs production and release of IL2 and IL2 induced TC activation

bottom line: anti-inflammatory that is used to tx things like psoriasis

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3
Q

Etanercept

A

recombinant form of TNF receptor that binds TNF-a

bottom line: anti-inflammatory that is used to tx things like psoriasis, RA, psoriatic arthritis

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4
Q

MTX

A

folate antimetabolite that reversibly binds to dihydrofolate reductase resulting in inhibition of purine and thymidylic acid synthesis

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5
Q

Ustekinumab

A

human monoclonal Ab targeting IL-12 and IL-23 –> inhibits activation of CD4 Th1 and Th17 cells

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6
Q

Foscarnet

A

pyrophosphate analog

indication: ganciclovir-resistant CMV

side effects: Ca chelation, renal wasting of Mg, dec release of PTH

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7
Q

Acyclovir

A

crystal nephropathy and neurotoxicity manifesting as delirium and/or tremor

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8
Q

Cidofovir

A

indication: CMV retinitis

side effects: nephrotoxicity (proteinuria and inc Cr)

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9
Q

Lamivudine

A

NRTI

side effects: rare, occasionally peripheral neuropathy and lactic acidosis

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10
Q

Sofosbuvir

A

inhibits nonstructural protein 5B, RNA-dependent RNA polymerase needed for HCV replication

Indication: HCV
SE: fatigue, nausea

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11
Q

Valganciclovir

A

ganciclovir prodrug

SE: severe neutropenia exacerbated by other BM suppressants (eg zidovudine, trimethoprim-sulfamethoxazole)

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12
Q

Ganciclovir

A

can cause severe neutropenia exacerbated by other BM suppressants (eg zidovudine, trimethoprim-sulfamethoxazole)

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13
Q

Loop diuretics

A

eg furosemide, bumetanide, torsemide

hypoK, hypoMg, hypoCa, ototoxicity

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14
Q

Thiazide diuretics

A

eg chlorthalidone, hydrochlorothiazide

act at distal convoluted tubule causing enhanced Na, Cl, and H2O excretion by blocking Na Cl symporters in DCT

hypoK, hypoNa, hyperuricemia, hypercalcemia

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15
Q

K+ sparing diuretics

A

eg triamterene, sprionolactone

act at collecting duct system

SE: hyperK

Spironolactone: gynecomastia, antiandrogen effects

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16
Q

Carbonic anhydrase inhibitors

A

eg acetazolamide

act at PCT and straight portion to block reabsorption of NaHCO3

SE: metabolic acidosis

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17
Q

Osmotic diuretics

A

eg mannitol

act at proximal tubule and descending limb of Loop of Henle to reduce Na and H2O reabsorption

SE: hyperNa, pulmonary edema

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18
Q

Metronidazole

A

tx anaerobic infections

indictations:

  • mild to moderate cases of c. diff (i.e. first and first recurrence)
  • Giardia lamblia
  • entamoeba histolytica
  • trichomonas vaginalis

more extensive absorption so less it delivered to distal colon than vanc and fidaxomicin

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19
Q

vancomycin

A

po for severe or recurrent c. diff colitis

bactericidal except at doses used to tx c. diff
- binds to terminal D-alanine residues of cell wall glycoproteins and prevents transpeptidases from forming cross-links

minimal systemic absorption

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20
Q

Fidaxomicin

A

macrocyclic abx

inhibits sigma subunit of RNA pol –> protein synthesis impairment and cell death
i.e. bacteriocidal activity

Advantages:

  • minimal systemic absorption
  • less effect on normal colonic flora than vanc or metronidazole
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21
Q

Doxycycline indications

A

clostridial skin infections (C perfringens, C septicum)

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22
Q

Neomycin

A

bacteriocidal

indications:

  • hepatic encephalopathy
  • diarrhea 2/2 e. coli
  • surgical pphx for GI procedures
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23
Q

chloroquine

A

tx of choice for sensitive plasmodium species

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24
Q

mefloquine

A

quinine analog

tx for chloroquine-resistant organisms

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25
Q

Primaquine

A

given for P. vivax and P. ovale with hypnozoites in addition to chloroquine or mefloquine

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26
Q

Ivermectin

A

tx for onchocerciasis (river blindness)

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27
Q

Mebendazole

A

anti-helminthic drug

indications:
- ascariasis
- trichuriasis
- hookworm
- pinworm infections

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28
Q

Nifurtimox

A

antiparasitic tx Chagas dz (American trypanosomiasis) caused by Trypanosoma cruzi

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29
Q

Pentamidine

A
  • pphyx for PCP PNA

- tx African sleeping sickness and leishmaniasis

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30
Q

Statin severe side effects

A
  • hepatitis
  • myopathy (i.e. serum CPK 10x normal and muscle pain) –> especially when combined with fibrates like gemfibrozil and fenofibrate bc they inc statin concentration
  • simvastatin = highest risk of myopathy, dose not to exceed 10 mg when concurrently giving fibrates
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31
Q

statin MoA

A

HMG-CoA redutase inhibitor

bile acid sequestrants can dec its absorption therefore dose at least 4 hrs apart

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32
Q

ezetimibe

A

dec cholesterol absorption in small intestine

inc risk of myopathy when given with statin but less than when statin given with fibrate

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33
Q

penicillin and cephalosporin MoA

A

irreversibly bind penicillin-binding proteins, e.g. transpeptidases which normally cross-link peptidoglycan in bacterial cell wall –> leads to cell wall instability and bacteriolysis

diff bacT species synthesize multiple diff penicillin-binding proteins

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34
Q

fluoroquinolones MoA

A

interfere with DNA replication by binding proteins like DNA gyrase in bacT (akin to topoisomerase II)

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35
Q

Macrolide MoA

A

binds ribosomal proteins

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36
Q

tetracyclines MoA

A

binds 30S ribosomal subunit preventing attachment of aminoacyl-tRNA

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37
Q

beta-lactamases

A

degrade penicillin and cephalosporins thereby preventing binding to pencillin-binding proteins

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38
Q

CTX resistance

A

structural changes in penicillin-binding proteins

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39
Q

Trimethoprim-sulfamethoxazole resistance

A

salvage metabolic pathway that circumvents metabolic pathway targeted by drug

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40
Q

Tetracyline and marcrolide resistance

A

transmembranous efflux pumps that prevent entry into the cell

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41
Q

aminoglycosides MoA

A

binds 30S and inhibits formation of initiation complex and causes misreading of mRNA

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42
Q

Chloramphenicol MoA

A

binds 50S and inhibits peptidyl transferase

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43
Q

macrolide MoA

A

binds 50S and prevents release of uncharged tRNA after it has donated its amino acid

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44
Q

Hydroxyurea

A

inhibits ribonucleotide reductase interfering with purine synthesis

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45
Q

6-mercaptopurine (6-MP)

A

blocks de novo purine synthesis

tx gout

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46
Q

5-fluorouracil (5-FU)

A

inhibits thymidylate synthase (decreases deoxythymidine monophosphate dTMP) interfering with purine synthesis

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47
Q

Methotrexate

A

inhibits dihydrofolate reductase (decreases dTMP) interfering with purine synthesis

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48
Q

Trimethoprim

A

inhibits bacterial dihydrofolate reductase (dec dTMP) interfering with purine synthesis

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49
Q

Trazodone

A

antidepressant

MoA =inhibits 5HT reuptake, alpha-adrenergic blockade, histamine H1 receptor antagonism

side effects = priapism (rare but severe), orthostatic HoTN, sedation

use cautiously when pt has condition predisposing to priapism = sickle cell, multiple myeloma

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50
Q

Tricyclic antidepressants

A

2nd line therapy

SE = cardiotoxicity

clomipramine = for OCD

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51
Q

Monoamine oxidase inhibitors

A

dietary restrictions bc of risk for hypertensive crisis (tyrosine, cheese)

Phenelzine = tx of resistant depression

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52
Q

SSRIs

A

sexual side effects = dec libido, anorgasmia, delayed ejaculation

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53
Q

SNRI

A

eg duloxetine

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54
Q

Zolpidem

A

non-benzo hypnotic used to tx insomnia

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55
Q

Clopidogrel

A

inhibits ADP-induced platelet aggregation

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56
Q

ACEi

A

tx of CHF, HTN, diabetic nephropathy

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57
Q

Indomethacin

A

non-specific COX inhibitor –> suppresses prostaglandin synthesis

promotes closure of PDA

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58
Q

Bosentan

A

competitive endothelin receptor antagonist used to tx idiopathic pulmonary arterial htn

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59
Q

vincristine

A

vinca alkaloid (also vinblastine)

MoA = inhibits microtubule formation by binding beta-tubulin and preventing polymerization

cell cycle-specific cytotoxicity during M phase (chromosomes can’t align and segregate)

toxicity = dose-dependent, most commonly PERIPHERAL NEUROPATHY

*chemotox man –> arms and legs

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60
Q

Topoisomerase I and II inhibitors

A

chemo drugs = irinotecan and etoposide

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61
Q

bleomycin

A

chemotherapeutic targeting G2 phase of cell cycle

MoA = intercalates with DNA and induces free radical formation

SE = lung fibrosis

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62
Q

doxorubicin

A

chemotherapeutic targeting G2 phase of cell cycle

MoA = intercalates with DNA and induces free radical formation

SE = irreversible dose-induced cardiomyopathy

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63
Q

cell-cycle nonspecific chemotherapeutic agents

A

cyclophosphamide = alkylating agent; SE include BM suppression, alopecia, hemorrhagic cystitis

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64
Q

Rifampin

A

inhibits bacT DNA-dependent RNA pol –> blocks DNA transcription

side effects: GI, Rash, Red-orange body fluids, cytopenia

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65
Q

Isoniazid

A

inhibits mycolic acid synthesis

mycolic acids normally cause mycobacteria to be acid-fast bc they retain the carbofuchsin dye and resist decoloration by acid-alcohol decolorizing agent –> when isoniazid inhibits it, it loses its acid-fast coloration and stop synthesizing new cell walls/proliferating

SE: neurotoxicity (give B6/pyridoxine), hepatotoxicity

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66
Q

Pyrazinamide

A

unclear MoA

SE: hepatotoxicity, hyperuricemia

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67
Q

Ethambutol

A

inhibition of arabinosyl transferase

SE: optic neuropathy

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68
Q

Amphotericin B

A

most toxic antifungal

tx for disseminated histoplasmosis

nephrotoxicity c/b dec in GFR and toxic effects on tubular epithelium –> increased permeability of distal tubule –> hypoK, hypoMg –> weakness and arrhythmias –> EKG shows T wave flattening, ST depression, U waves, PAC, PVC –> profound hypoK get vtach or vfib

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69
Q

glucocorticoids and osteoporosis

A
  • inc osteoclast differentiation and activity
  • dec osteoblast activity
  • inhibiting intestinal action of Vit D in promoting Ca absorption
  • inc PTH levels

occurs if taken daily for >6 mo

can also occur with topical intake, eg inhaler

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70
Q

Meds associated with osteoporosis

A
  1. anticonvulsants that induce CYP450 - phenobarb, phenytoin, carbamazepine. inc vit D catabolism
  2. aromatase inhibitors - dec estrogen
  3. medroxyprogesterone - “
  4. GnRH agonists - dec testosterone and estrogen
  5. PPIs - dec Ca absorption
  6. unfractionated heparin - dec bone formation
  7. glucocorticoids - “
  8. thiazolidinediones - “
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71
Q

Tx for hyperammonemia

A

benzoate or phenylbutyrate = bind aa and lead to excretion

lactulose = acidifies GI tract and traps NH4+ so you poop it out

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72
Q

volume of distribution (Vd)

A

Vd = amount of drug in body / plasma drug concentration

theoretical fluid volume required to maintain total absorbed drug amount at the plasma concentration

Vd of plasma protein-bound drug can be altered by liver and kidney disease (dec protein binding inc Vd)

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73
Q

half-life (t1/2)

A

0.7 x Vd
________
Clearance

a drug infused at a constant rate takes 4-5 half-lives to reach steady state

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74
Q

Clearance (CL)

A

rate of drug elimination = Vd x Ke (elimination constant)
____________________
plasma drug concentration

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75
Q

Loading dose

A

Cp X Vd / F

Cp = target plasma concentration

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76
Q

Maintenance dose

A

Cp x CL / F

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77
Q

Zero-order elimination

A

constant amount of drug-eliminated per unit time

Cp dec linearly with time

e. g. PEA (round like 0)
- Phenytoin
- Ethanol
- Aspirin

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78
Q

First-order elimination

A

constant fraction of drug eliminated per unit time

Cp dec exponentially with time

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79
Q

Phase I metabolism

A

Reduction, oxidation, hydrolysis with P450 –> slightly polar water-soluble metabolites (still active usually)

Geriatric patients lose this first

80
Q

Phase II metabolism

A

Conjugation (Glucuronidation, Acetylation, Sulfation) –> very polar, inactive metabolites that are renally excreted

Geriatric patients have GAS

slow acetylators –> greater side effects bc it dec rate of metabolism

81
Q

Competitive antagonist

A

shifts curve to the right –> dec potency, no change in efficacy

can overcome by inc concentration of agonist substrate

e.g. Diazepam + flumazenil on GABA receptor

82
Q

Noncompetitive antagonist

A

shifts curve down –> dec efficacy

can’t be overcome by inc agonist substrate

e.g. NE + phenoxybenzamine on alpha receptor

83
Q

Partial agonist

A

acts at same site as full agonist, but with reduced maximal effect –> dec efficacy

potency is variable and can be inc or dec

e.g. morphine (full agonist) + buprenorphine (partial agonist) at opioid mu-receptor

84
Q

Therapeutic index

A

LD50/ED50

median lethal dose / median effective dose

85
Q

what two systems are part of the SNS but innervated by cholinergic neurons?

A

Adrenal medulla

Sweat glands

86
Q

Nicotinic ACh receptors

A

ligan-gated Na/K channels

Nn found in autonomic ganglia
Nm found in NMJ

87
Q

Muscarinic ACh receptors

A

GPCRs acting through 2nd messengers

5 subtypes:
M1-5

88
Q

alpha-1 receptors

A

G-protein class: q

Major functions:

  • inc vascular smooth muscle contraction
  • inc pupillary dilator muscle (mydriasis)
  • inc intestinal and bladder sphincter muscle contraction (i.e. can’t go to bathroom when running from a bear)
89
Q

alpha-2 receptors

A

G-protein class: i

Major functions:

  • dec sympathetic outflow
  • dec insulin release
  • dec lipolysis
  • inc platelet platelet aggregation
90
Q

beta-1 receptors

A

G-protein class: s

Major functions:

  • inc heart rate
  • inc contractility
  • inc renin release
  • inc lipolysis
91
Q

beta-2 receptors

A

G-protein class: s

Major functions:

  • vasodilation
  • bronchodilation
  • inc heart rate
  • inc contractility
  • inc lipolysis
  • inc insulin release
  • dec uterine tone (tocolytic)
  • ciliary muscle relaxation
  • inc aqueous humor production –> hence can use for glaucoma
92
Q

M1 receptors

A

G-protein class: q

Major functions:

  • CNS
  • enteric nervous system
93
Q

M2 receptors

A

G-protein class: i

Major functions:

  • dec HR
  • dec contractility of atria
94
Q

M3 receptors

A

G-protein class: q

Major functions:

  • inc exocrine gland secretions (eg lacrimal, gastric acid)
  • inc gut peristalsis
  • inc bladder contraction
  • bronchoconstriction
  • inc pupillary sphincter muscle contraction (miosis)
  • ciliary muscle contraction (accomodation)
95
Q

D1 receptors

A

G-protein class: s

Major functions:
-relaxes renal vascular smooth muscle

96
Q

D2 receptors

A

G-protein class: i

Major functions:
-modulates transmitter release especially in the brain

97
Q

H1 receptors

A

G-protein class: q

Major functions:

  • inc nasal and bronchial mucus production
  • contraction of bronchioles
  • pruritus
  • pain
98
Q

H2 receptors

A

G-protein class: s

Major functions:
-inc gastric acid secretion

99
Q

vasopressin 1 (v1) receptor

A

G-protein class: q

Major functions:
-inc vascular smooth muscle contraction

100
Q

vasopressin 2 (v2) receptor

A

G-protein class: s

Major functions:
-inc H2O permeability and reabsorption in collecting tubules of the kidney

i.e. this is were vasopressin = ADH acts

V2 is found in the two kidneys

101
Q

Bethanechol

A

direct cholinergic agonist

Postoperative ileus, neurogenic ileus, urinary retention

  • activates bowel and bladder smooth muscle
  • resistant to AChE
102
Q

Carbachol

A

direct cholinergic agonist

Glaucoma, pupillary contraction, relief of intraocular pressure

carbon copy of acetylcholine

103
Q

Pilocarpine

A

direct cholinergic agonist

potent stimulator of sweat, tears, saliva, open-angle and closed-angle glaucoma

  • contracts ciliary muscle of eye (open-angle glaucoma)
  • contracts pupillary sphincter (closed-angle glaucoma)
  • resistant AChE
104
Q

Methacholine

A

direct cholinergic agonist

challenge test for dx of asthma

stimulates muscarinic receptors in airway when inhaled

105
Q

Neostigmine

A

indirect choline agonist, i.e. anticholinesterase

postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of NMJ blockade (postop)

inc endogenous ACh
Neo CNS = No CNS penetration

106
Q

Pyridostigmine

A

indirect choline agonist, i.e. anticholinesterase

myasthenia gravis (long acting); doesn’t cross BBB

inc endogenous ACh, inc strength

107
Q

Edrophonium

A

indirect choline agonist, i.e. anticholinesterase

Dx of myasthenia gravis (extremely short acting)

inc endogenous ACh

108
Q

Physostigmine

A

indirect choline agonist, i.e. anticholinesterase

anticholinergic toxicity (crosses BBB)

inc endogenous ACh

“Physostigmine phyxes atropine overdose”

109
Q

Donepezil

A

indirect choline agonist, i.e. anticholinesterase

Alzheimer’s disease

inc endogenous ACh

110
Q

what do you look out for in predisposed patients with all cholinomimetic agents?

A

COPD exacerbation
asthma
peptic ulcers

111
Q

Cholinesterase inhibitor poisoning

A

organophosphates e.g. parathion

irreversibly inhibit AChE

sx: DUMBBBELSS
- Diarrhea
- Urination
- Miosis
- Bronchospasm
- Bronchorrhea
- Bradycardia
- Excitation of skeletal muscle and CNS
- Lacrimatoin
- Sweating
- Salivation

antidote = atropine and pralidoxime (regenerates active AChE)

112
Q

Benztropine

A

antimuscarinic

use for Parkinson’s (improves tremor) and dystonia 2/2 antipsychotics

113
Q

Scopolamine

A

antimuscarinic

use for motion sickness

114
Q

oxybuynin

A

antimuscarinic

use to reduce urgency in mild cystitis and reduce bladder spasms

115
Q

glycopyrrolate

A

antimuscarinic - decrease GI and respiratory secretions

Parenteral: preop use to reduce airway secretions

PO: drooling, peptic ulcers

116
Q

Atropine toxicity = anticholinergic toxidrome

A 
Hot as a hare
Dry as a bone
Red as a beet
Blind as a bat
Mad as a hatter

Jimson weed (Datura) –> gardener’s pupil mydriasis due to plant alkaloids)

117
Q

Epinephrine selectivity

A

non-selective alpha

118
Q

NE selectivity

A

non-selective alpha activity, some beta1 activity

tx HoTN but dec renal perfusion

119
Q

Isoproterenol selectivity

A

non-selective beta activity

tx torsade de pointes (tachycardia dec QT interval), bradyarrhythmias (but can worsen ischemia)

120
Q

Dopamine selectivity

A

high dose - non-selective alpha
medium dose - B1 > B2
low dose - DA activity

tx shock (renal perfusion), heart failure

  • inotropic
  • chronotropic
121
Q

Dobutamine selectivity

A

low alpha activity

B1&raquo_space; B2

tx heart failure, cardiac stress testing

  • inotropic
  • chronotropic
122
Q

phenylephrine selectivity

A

alpha 1 > alpha 2

tx HoTN, ocular procedures (mydriatic), rhinitis

123
Q

albuterol, salmeterol, terbutaline selectivity

A

beta 2&raquo_space; beta 1

124
Q

ritodrine selectivity

A

beta 2

tocolytic

125
Q

beta1 and reflex activity of isoproterenol

A

little alpha effect but causes beta2-mediated vasodilation –> dec mean arterial pressure and inc heart rate

vs.

NE:
inc systolic and diastolic pressure through alpha1-mediated vasoconstriction –> inc MAP –> bradycardia

126
Q

sympathoplegics

A

clonidine and alpha-methyldopa

centrally acting alpha2-agonists –> dec central sympathetic outflow

use for HTN especially with renal disease since you don’t get decreased perfusion to kidney like you do with alpha1 agonism

127
Q

Phenoxybenzamine

A

irreversible nonselective alpha blockade

use prior to pheochromocytoma resection because released catecholamines won’t overcome block

128
Q

epinephrine vs phenylephrine

A

epinephrine = beta > alpha blockade therefore when you do alpha blockade you actually get a reversal (net decrease) in mean blood pressure because of beta2 action when you administer E

phenylephrine = just alpha blockade therefore when you co-administer with an alpha blocker you see a suppression of the mean arterial pressure to normal without phenylephrine but not a reversal (net decrease) like you see with E

129
Q

beta blockers and MI

A

decreases mortality

130
Q

beta blockers and SVT

A

metoprolol, esmolol

dec AV conduction velocity = class II antiarrhythmic

131
Q

HTN and beta blockers

A

beta1 receptor blockade on JGA cells

132
Q

beta1-selective antagonists

A

A BEAM of beta1 blockers.

Use for patients with comorbid pulmonary disease

Acebutolol (partial agonist)
Betaxolol
Esmolol (short acting)
Atenolol
Metoprolol
133
Q

Nonselective beta antagonists

A

Please Try Not Being Picky

Propranolol
Timolol
Nadolol
Pindolol

134
Q

Nonselective (vasodilatory) alpha and beta antagonists

A

carvedilol and labetalol

135
Q

Partial beta Agonists

A

PAPA

Pindolol
Acebutolol

136
Q

Digitalis antidote

A

K+ normalization
Lidocaine
Anti-dig Fab fragments
Mg2+

137
Q

Lead antidote

A

CaEDTA
Dimercaprol
Succimer
Penicillamine

138
Q

Cyanide antidote

A

Nitrite + thiosulfate

hydroxocobalamin

139
Q

Heparin antidote

140
Q

tPA, streptokinase, urokinase antidote

A

aminocaproic acid

141
Q

what drugs cause torsades de pointes?

A

class III (sotalol) and class IA (quinidine) antiarrhythmics

142
Q

what drugs cause agranulocytosis?

A

Agranulocytosis Could Certainly Cause Pretty Major Damage

Clozapine
Carbamazepine
Colchicine
Propylthiouracil
Methimazole
Dapsone
143
Q

what drugs cause hemolysis in G6PD deficient patients?

A

oxidizing drugs

Isoniazid
Sulfonamides
Primaquine
Aspirin
Ibuprofen
Nitrofurantoin
144
Q

what drugs cause megaloblastic anemia?

A

Having a blast with PMS

Phenytoin
MTX
sulfa drugs

145
Q

what drugs cause pulmonary fibrosis?

A

Bleomycin
Amiodarone
Busulfan

146
Q

what drugs cause focal to massive hepatic necrosis?

A

Halothane
Amanita phalloides
Valproic acid
Acetaminophen

147
Q

what drugs cause pseudomembranous colitis?

A

Clindamycin

ampicillin

148
Q

what drugs cause gynecomastia?

A

Some Drugs Create Awkward Knockers

Spironolactone
Digitalis
Cimetidine
chronic Alcohol use
estrogens
Ketoconazole
149
Q

what drugs cause hyperglycemia?

A 
Niacin
tacrolimus (immunosuppressant)
protease inhibitors
HCTZ
corticosteroids
150
Q

what drugs cause gout?

A

furosemide
thiazides
niacin
cyclosporine

151
Q

what drugs cause myopathies?

A

Fish N CHIPS Give you myopathies

Fibrates
Niacin
Colchicine 
Hydroxychloroquine 
Interferon-alpha
Penicillamine
Statins 
Glucocorticoids
152
Q

what drugs cause Stevens-Johnson syndrome?

A 
Penicillin
Ethosuximide
Carbamazepine
Sulfa drugs
Lamotrigine
Allopurinol 
Phenytoin
Phenobarbital

Bad rash after a PEC SLAPP

153
Q

what drugs cause SLE-like syndrome?

A

Hydralazine
INH
Procainamide
Phenytoin

It’s not HIPP to have lupus.

154
Q

what drugs cause tendonitis, tendon rupture and cartilage damage?

A

fluoroquinolones

155
Q

what drugs cause diabetes insipidus?

A

demeclocycline, Lithium

156
Q

what drugs cause seizures?

A

“with seizures I BITE My tongue”

Isoniazid
Bupropion 
Imipenem/cilastatin
Tramadol
Enflurane
Metoclopramide
157
Q

what drugs cause a disulfiram-like reaction?

A

metronidazole
certain cephalosporins
procarbazine
1st generation sulfonylureas

158
Q

what drugs cause nephrotoxicity/ototoxicity?

A

aminoglycosies
vancomycin
loop diuretics
cisplatin

159
Q

P450 inducers

A

“Momma Barb Steals Phen-phen and Refuses Greasy Carbs Chronically”

Modafinil
Barbiturates
St. John's wort
Phenytoin
Rifampin
Griseofulvin
Carbamazepine 
Chronic alcohol use
160
Q

P450 Inhibitors

A

“MACIG RACKS in GQ”

Macrolides
Amiodarone
Grapefruit juice
Isoniazid
Cimetidine
Ritoniavir
Acute Alcohol abuse
Ciprofloxacin 
Ketoconazole
Sulfonamides
Gemfibrozil
Quinidine
161
Q

Sulfa drugs

A

Popular FACTSSS

Probenecid
Furosemide
Acetazolamide
Celecoxib
Thiazides
Sulfonamide abx
Sulfasalazine
Sulfonylureas

sx of allergy = fever, UTI, rash, SJS, hemolysis, thrombocytopenia, agranulocytosis, hives

162
Q

-triptan

A

5-HT 1B/1D agonists used for migraines

163
Q

-azine

A

Phenothiazine (neuroleptic, antiemetic)

e.g. chlorpromazine

164
Q

-oxin

A

cardiac glycoside = inotropic agent

eg digoxin

165
Q

what drug is protective against diabetic nephropathy?

166
Q

Hydralazine

A

inc cGMP –> smooth muscle relaxation

vasodilation of arterioles > veins –> afterload reduction

first-line therapy for HTN in pregnancy with methyldopa
- give beta-blocker to prevent reflex tachycardia

SE: compensatory tachycardia (don’t give with angina/CAD), fluid retention, nausea, HA, angina, Lupus-like syndrome

167
Q

nitroprusside

A

short-acting, inc cGMP via direct release of NO

look out for cyanide toxicity

168
Q

Fenoldopam

A

dopamine D1 receptor agonist - coronary, peripheral, renal, splanchnic vasodilation

dec BP, inc natriuresis

169
Q

HMG-CoA MOA

A

inhibit conversion of HMG-CoA to mevalonate = cholesterol precursor

170
Q

niacin as lipid-lowering agent

A

inhibits lipolysis in adipose tissue; reduces hepatic VLDL secretion into circulation

171
Q

bile acid resins MoA

A

cholestyramine, colestipol, colesevelam

prevent intestinal reabsorption of bile acids –> liver has to use cholesterol to make more

SE = dec absorption of fat-soluble vitamins, cholesterol gallstones

172
Q

cholesterol absorption blockers

A

ezetimibe

prevent cholesterol absorption at small intestine brush border

173
Q

drugs that inc HDL

A

HMG-CoA
Niacin
slightly bile acid resins
fibrates

174
Q

drugs that dec TG the most

A

fibrates (gemfibrozil, clofibrate, bezafibrate, fenofibrate)

175
Q

Digoxin toxicity findings including EKG

A

half-life = 40 hours, excreted in urine

cholinergic - n/v/d, blurry yellow vision

EKG - inc PR, dec QT, ST scooping, T inversion, arrhythmia, AV block

hyperkalemia = poor prognosis

factors predisposing to toxicity:

  • renal failure
  • hypokalemia (permissive for digoxin binding at K binding site on NaK ATPase)
  • quinidine (dec digoxin clearance, displaces digoxing from tissue-binding sites)
176
Q

Class I antiarrhythmics

A

Na channel blockers

  • local anesthetics
  • block or slow conduction
  • dec slope of phase 0 depolarization
  • inc threshold for firing in abnormal pacemaker cells
  • state dependent - selectively depresses more frequently depolarized tissue, e.g. tachycardia
  • hyperkalemia causes inc toxicity
177
Q

Class IA

A

“The Queen Proclaims Diso’s Pyramid”
Quinidine, Procainamide, Disopyramide

MoA: inc AP duration, inc effective refractory period

Indication: atrial and ventricular arrhythmias, especially reentrant and ectopic SVT and VT

Toxicity:
quinidine - HA, tinnitus
procainamide - reversible SLE-like syndrome
disopyramide - heart failure
general - thrombocytopenia, torsades due to inc QT interval

178
Q

Class IB

A

“I’d Buy Lidy’s Mexican Tacos”
Lidocaine, Mexiletine, Tocainide

MoA: dec AP duration; Preferentially affect ischemic or depolarized Purkinje and ventricular tissue

Indication: acute ventricular arrhythmias esp POST-MI and in digitalis-induced arrhythmias

toxicity: local anesthetic, CNS stimulation/depression, CV depression

179
Q

Class IC

A

Flecainide, propafenone

MoA: No effect on AP duration. Useful in ventricular tachycardias that progress to VF and in intractable SVT.

Indication: last reosrt in tachyarrhythmias. For pts without structural abnormalities.

IC is Contraindicated in structural heart disease and post-MI!!!

Toxicity: proarrhythmic, especially post-MI. Significantly prolongs refractory period in AV node

180
Q

Class II

A

beta-blockers: metoprolol, propranolol, esmolol, atenolol, timolol

MoA: dec SA and AV node activity by dec cAMP, dec Ca currents. dec slope of phase 4

indicated for Vtach, SVT, slowing ventricular rate during a-fib and a-flutter

toxicity: impotence, exacerbation of asthma, CV effects (bradycardia, AV block, CHF), CND effects (sedation, sleep alterations). may mask signs of hypoglycemia.

metoprolol can cause dyslipidemia. tx overdose with glucagon.

Propranolol can exacerbate Prinzmetal’s angina.

181
Q

Class III

A

“AIDS”: amiodarone, ibutilide, dofetilide, sotalol

MoA: inc AP duration, inc effective refractory period

indication: when other antiarrhythmics fail. inc QT interval

toxicity:
- sotalol-torsades, excessive beta block
- ibutilide - torsades
- amiodarone - pulmonary fibrosis, hepatotoxicity, hypothyroidism/hyperthyroidism, corneal deposits, skin deposits (blue/gray) leading to photodermatitis, neuro effects, constipation, CV effects (bradycardia, heart block, CHF)

amiodarone = class I, II, III, IV effects bc it alters the lipid membrane –> check PFTs, LFTs, and TFTs

182
Q

Class IV

A

calcium channel blockers: verapamil, diltiazem

MoA: dec doncution velocity, inc effective refractory period, inc PR interval

indication: prevention of nodal arrhythmias, eg SVT
toxicity: constipation, flushing, edema, CV (CHF, AV block, SA depression)

183
Q

Adenosine

A

inc K out of cells –> hyperpolarizes cell and dec Ca current

indication: SVT, short acting (~15 sec)
toxicity: flushing, hypotension, chest pain

effects blocked by theophylline and caffeine

184
Q

Mg as antiarrhythmic

A

effective in torsades and digoxin toxicity

185
Q

Biguanides

A

eg metformin

inc insulin sensitivity

SE: lactic acidosis (contraindicated in renal failure)

186
Q

Sulfonylureas

A

eg. Tolbutamide, Glyburide, Glipizide

close K channel in beta cell membrane –> depol -> inc [Ca}i –> insulin release

*requires some islet cell fxn therefore can’t use in DM1

187
Q

Glitazones / thiazolidinediones

A

eg Pioglitazone, rosiglitazone

  • inc insulin sensitivity in peripheral tissues
  • binds PPAR-gamma nuclear transcription regulator (fatty acid storage and glucose metabolism, activation causes inc insulin sensitivity and adiponectin)

SE: weight gain, edema, hepatotoxicity

188
Q

alpha-glucosidase inhibitors

A

acarbose, miglitol

inhibits intestinal brush border alpha-glucosidases –> delayed sugar hydrolysis and glucose absorption –> dec postprandial hyperglycemia

189
Q

amylin analogs

A

pramlintide

dec glucagon

used in DM 1 and 2

SE: hypoglycemia, n/d

190
Q

glp-1 analogs

A

exenatide, liraglutide

inc insulin, dec glucagon release

used only in type 2 DM

SE: n/v, pancreatitis

191
Q

DPP-4 inhibitors

A

linagliptin, saxagliptin, sitagliptin

inc insulin, dec glucagon release

only used in DM2

SE: mild urinary and respiratory infections

192
Q

Propylthiouracil, methimazole

A

block peroxidase –| organification of iodide and coupling of thyroid hormone synthesis, i.e. I- to I2

propyl also –| 5’deiodinase which is responsible for conversion of T4 to T3 peripherally

SE: skin rash, rarely AGRANULOCYTOSIS, aplastic anemia, hepatotoxicity (propylthiouracil).

Methimazole also a possible TERATOGEN.

193
Q

Levothyroxine, triiodothyronine

A

hypothyroidism, myxedema

se: tachycardia, heat intolerance, tremors, arrhythmias

194
Q

octreotide indications

A

acromegaly, carcinoid, gastrinoma, glucagonoma, esophageal varices

195
Q

Demeclocycline toxicity

A

used for SIADH bc it is an ADH antagonist

can cause nephrogenic DI, photosensitivity, abnormalities of bone and teeth (bc it’s a member of tetracycline family)

196
Q

glucocorticoid mechanism of action

A

dec production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2

197
Q

Ticlopidine and clopidogrel

A

irreversible blockade of ADP receptor (responsible for helping platelet adhere to endothelium and inducing GpIIb/IIIa expression)

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