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.Pharmacology > TO RECALL 1 > Flashcards

TO RECALL 1 Flashcards

1
Q

Drug:

AMIODARONE

A
  • drug for cardiac arrythmias
  • has multiple receptors (i.e. nuclear thyroid hormone receptor) - contributes to its toxicity
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2
Q

Drug:

SOTALOL

A
  • Beta-blocker
  • used as an anti-arrythmic
  • Given as a racemic mixture where both L- and D- enantiomers are equipotent K+ channel blockers BUT L- as the more potent Beta-adrenergic antagonist

Example for The Specificity of Drug Responses

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3
Q

Drug:

Nitrovasodilators

A
  • treats angina where NO-dependent elevation of cGMP in vascular smooth muscle produces vasodilation
  • chronic administaration results in complete tolerance (Tachyphylaxis)
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4
Q

Drug:

VARENICLINE

A
  • used for smoking cessation therapy
  • partial agonist of nicotinic receptors
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5
Q

Drug:

SIDENAFIL, TADALAFIL, VARDENAFIL

A
  • phosphodiesterase (PDE) 5 inhibitors
  • in vasculature
  • SIDENAFIL - treatment for erectile dysfunction
  • co-administration with nitrovasodilators can cause catastrophic vasodilation & severe hypotension
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6
Q

Drug:

WARFARIN

A
  • oral anticoagulant
  • has a narrow margin between therapeutic inhibiton of clot formation and bleeding complications
  • Antibiotics (decrease vit. K absorption) & NSAIDS (i.e. Aspirin that inhibits platelet aggregation) will enhance effect of warfarin - AT RISK FOR BLEEDING
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7
Q

Drug:

ALPHA-METHYL TYROSINE

A
  • inhibits synthesis of norepinephrine
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8
Q

Drug:

COCAINE

A
  • BLOCKS Norepinephrine uptake
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9
Q

Drug:

AMPHETAMINE

A
  • promotes NE release
  • similar effect to cocaine
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10
Q

Drug:

SELEGILINE

A
  • inhibits NE breakdown by MAO (Monoamine Oxidase)
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11
Q

Drug:

FUROSEMIDE, CHLOROTHIAZIDE, AMILORIDE

A
  • Diuretics
  • affects ion pumps & transporters to increase movement of Na+ into the urine
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12
Q

Drug:

OMEPRAZOLE

A
  • Proton pump inhibitor (H+-K+ ATPase)
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13
Q

Drug:

TERBUTALINE

A
  • Beta 2 adrenergic agonist
  • used for broncodilation in asthma
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14
Q

Drug:

Sulfonylureas & Meglitinides

A
  • oral hypoglycemic drug (lowers blood sugar)
  • activate Beta cells to increase insulin release in pancreas
  • used in treatment of type II diabetes mellitus

Sulfonylureas - target ATP-sensitive potassium channels
Meglitinides - target sulfonylurea receptor 1 (SUR1)

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15
Q

Drug:

LIDOCAINE & TETRACAINE

A
  • Local anesthetics
  • block voltage-gated Na+ channels in pain neurons to inhibit depolarization
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16
Q

Drug:

NIFEDIPINE, DILTIAZEM, VERAPAMIL

A
  • Ca+ channel antagonist/blockers
  • blocks muscle contraction in blood vessels leading to vasodilation
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17
Q

Drug:

ROCURONIUM

A
  • competitive antagonist of acetylcholine
  • Muscle Relaxant
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18
Q

Drug:

NESIRITIDE

A
  • Synthetic BNP agonist
  • used in treatment of acute decompensated heart failure
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19
Q

Drug:

SACUBITRIL

A
  • neprilysin inhibitor
  • blocks ANP & BNP breakdown
  • treats decompensated heart failure
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20
Q

Drug:

ATROPINE

A
  • blocks acetylcholine (parasympathetic ligand)
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21
Q

Drug:

DOBUTAMINE

A
  • Beta 1 receptor agonist
  • increase strength of heart contractions
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22
Q

Drug:

TETRABENZINE

A
  • Symptomatic treatment for your Huntington disease - Antichorea (chorea: movement disorder)
  • inhibits (SLC18A2) VMAT2: Vesicular monoamine transporter - function to store amines (i.e. Dopamine)
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23
Q

Drug:

CANAGLIFLOZIN, DAPAGLIFLOZIN, EMPAGLIFLOZIN

A
  • Inhibits SLC5 family transporters SGLT1 & SGLT2 (Na+-glucose transporters)
  • treatment for diabetes
  • reduces renal reabsorption of glucose, leading to glucose elimination

at the proximal convoluted tubules

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24
Q

Drug:

LESINURAD

A
  • Treatment for gout
  • targets (SLC22A12) URAT1 (Uric Acid Transporter 1) to inhibit uric acid reabsorption in the kidney

at the proximal convoluted tubules

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25
Q

Drug:

IVACAFTOR

A
  • used in treatment for cystic fibrosis
  • a potentiator that increases the probability that the mutant chloride channel (CFTR-G551D) remains open
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26
Q

Drug:

PARAVASTATIN

A
  • HMG-CoA reductase Inhibitor
  • used to reduce amount of ‘bad cholesterol’
  • functions through uptake by SLC OATP1B1 in liver
  • when it does not enter the liver, an adverse response is skeletal muscle myopathy
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27
Q

Drug:

LOPERAMIDE

A
  • Peripheral opioid
  • for diarrhea
  • Do not mix with Quinidine (potent Pgp inhibitor)
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28
Q

Drug:

QUINIDINE

A
  • anti-arrythmia
  • Potent Pgp inhibitor
29
Q

Transporter:

Pgp or MDR1

A

P-glycoprotein or Multidrug Resistance Protein 1

  • works to eliminate drugs via powerful efflux mechanisms
  • usually for protection (common in BBB) but pathogenic when present in tumor cells
30
Q

Drug:

SSRI - Selective Serotonin Reuptake inhibitor

A
  • anti-depressants
  • targets SERT (Serotonin Transporter) or SLC 6A4
31
Q

Drug:

TIAGABINE

A
  • anti-epileptic drug
  • inhibits GABA reuptake by interacting with GAT1 (GABA transporter in the brain) to prolong GABA in the synaptic cleft
32
Q

Drug:

FEXOFENADINE

A
  • antihistamine drug: H1 receptor antagonist

Uptake: in liver by OATP1B1 and OATP1B3
Excretion: in bile by MRPT2 and BSEP

33
Q

Drug:

BOSENTAN

A
  • an endothelin antagonist
  • treatment for pulmonary arterial hypertension
  • Cyclosporine, rifampicin, sidenafil inhibits its uptake

Uptake: OATP1B1 and OATP1B3
Metabolized by: CYPC9 and CYP3A4

34
Q

Drug:

RIFAMPICIN

A
  • treats tuberculosis infection
35
Q

Drug:

ACETAMINOPHEN

A
  • non-opioid analgesic and antipyretic agent used to treat fever and mild to moderate pain
  • aka Paracetamol
36
Q

Drug:

VALPROIC ACID

A
  • anticonvulsant (or anti-epileptic)
37
Q

Poisoning-Antidote: What is the antidote for?

Acetaminophen

A

N-Acetylcysteine

38
Q

Poisoning-Antidote: What is the antidote for?

Organophosphorus and carbamate
(in pesticides)

A

Atropine Sulfate

39
Q

Poisoning-Antidote: What is the antidote for?

Iron

A

Deferoxamine

40
Q

Poisoning-Antidote: What is the antidote for?

Lead

A
  • EDTA
  • CaNa2
41
Q

Poisoning-Antidote: What is the antidote for?

Methanol, ethylene glycol

A
  • ethanol
  • fomepizole
42
Q

Poisoning-Antidote: What is the antidote for?

Cyanide

A
  • Thiosulfate
  • sodium
  • Hydroxocobalamine
  • hydrochloride
43
Q

Poisoning-Antidote: What is the antidote for?

Carbon monoxide

A

Oxygen

44
Q

Poisoning-Antidote: What is the antidote for?

Opioids

A

Naloxone hydrochloride

45
Q

Poisoning-Antidote: What is the antidote for?

Coumarin, indanedione

A

Vitamin K (phytonadione)

46
Q

Isoniazid is metabolized by what enzyme? What are the enzyme’s gene variations?

A

N-acetyl transferase 2 (NAT2)

NAT2 gene can result to 3 variations of acetylators : (1) fast acetylator, (2) intermediate acetylator, (3) slow acetylator

slow acetylators are associated with hepatotoxicity

47
Q

Drug

Primaquine

A

Anti malaria drug

First pharmacogenetics discovery where primaquine induces hemolysis in patients with G6PD deficiency leading to anemia

48
Q

Drug

Thiopental

A

Anesthetic - very lipophilic

49
Q

2 most important phase 2 reactions and why

A
  • glucuronidation - most dominant phase in adults
  • sulfation - only phase 2 reactions in neonates
50
Q

Major enzyme family for Phase 1 metabolism - what is the most common enzyme from that family

A

CYP 450 - CYP3A4

51
Q

Drug

Anastrozole

A

Drug to treat estrogen dependent tumors
It inhibits CYP19/aromatase which functions to produce estrogen from testosterone (metabolizes testosterone and androstenedione)

52
Q

Most polymorphic CYP450 enzyme - be conservative with associated drugs

A

CYP2D6

53
Q

Drugs metabolized by FMO3

A
  • nicotine
  • ranitidine & cimetidine (H2 antagonists/blockers)
  • clozapine (antipsychotics)
  • itopride (antiemeptics)
54
Q

Drug

Carbamazepine

A

Anti epileptic drug

Metabolized by microsomal EHs to dihydrodiol for inactivation
*Valnoctamide (tranquilizer) and Valproate (anticonvulsant) inhibits mEH which leads to carbamazepine toxicity

55
Q

sEH - soluble Epoxide hydrolase

A

Epoxides of arachidonic acid and docosahexaenoic acid reduce inflammation, hypertension, and pain but are normally degraded quickly by sEH to vicinal diols that are generally less biologically active

sEH inhibitors reduce both inflammatory and neuropathic pain and synergize with nonsteroidal anti-inflammatory drugs

56
Q

Drug

IRINOTECAN

A

Cancer chemotherapeutic agent

Metabolized by intracellular carboxylesterases

57
Q

What drug is more pharmacologically active than the parent after phase 2 metabolism

A

Morphine (glucuronide conjugate)
Minoxidil ( sulfate conjugate)

58
Q

Only phase 2 reaction that occurs in the ER (like phase 1) instead of the cytosol (normal for phase 2)

A

Glucuronidation

59
Q

Crigler-Najjar Syndroe

A

Defect in UGT enzyme (glucuronidation)

Type 1 - complete lack
Type 2 - deficiency

60
Q

Gilbert Syndrome

A

Mutation in the UGT1A1 gene

Indications:
- predisposed to adverse drug reactions
- reduced capacity to metabolize drugs by UGT1A1

61
Q

Sulfation as Phase 2 metabolism reaction

Sulfotransferase (SULT) more abundant in intestine than liver

A

SULT1B1

SULT1A1 is most important in the liver

62
Q

Sulfation as Phase 2 metabolism reaction

SULT enzyme in human fetal tissues

A

SULT1C1

63
Q

Sulfation as Phase 2 metabolism reaction

SULT in skin that catalyzes cholesterol

A

SULT2B1b

64
Q

NAPQI (N-acetyl-p-benzoquinone imine)

A

Toxic metabolite of acetaminophen; neutralized through conjugation with GSH (reduced form of glutathione)

65
Q

Phase 2 reaction that protects cellular macromolecules from damage against reactive electrophiles

A

Glutathione Conjugation/ Glucuronidation

GSTs catalyze the transfer of glutathione to reactive electrophile

Over expression of GSTs is related to resistance to apoptosis and reduced efficacy of chemotherapy - inhibition of GSTs is used to modulate drug resistance by sensitizing tumors to anticancer drugs

66
Q

Drug

Isoniazid

A

Antibiotic (common for TB)

67
Q

Drug

Dextromethorphan

A

Cough suppressant

68
Q

Enzyme Induction vs. Enzyme Inhibition

Drug A is the inducer of enzyme; Drug B is the one being
metabolized by the enzyme. Drug B will be metabolized faster and it becomes less effective if it is coadministered with Drug A

A

.Pharmacology (55 decks)

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