Primer 21 - Drug Metabolism Flashcards

1
Q

Which metabolites does yield from phase I?

A

1) Sightly polar. 2) Water-soluble. 3) Active.

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2
Q

Which are the reaction and metabolites yield from phase II?

A

Reactions (conjugation): Glucuronidation, Acetylation and Sulfation “GAS”.
Metabolites: Very polar and inactive.

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3
Q

Which is the phase that geriatric patients lose?

A

Phase I, Geriatric patients have GAS (phase II).

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4
Q

Which cytochrome performance phase I reactions?

A

Cytochrome P-450 in liver.

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5
Q

What kind of patients are more susceptibles for high side effects?

A

Patients who are slow acetylators have increase side effects from certain drugs because of decrease rate of metabolism.

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6
Q

What is happened when two drugs have the same metabolism by Cytochrome P-450?

A

Drug-drug interaction, one of them drugs going to increase in serum plasma levels or prolong the action.

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7
Q

What is the subfamily type of CYP3A4?

A

CYP (Cytochrome) 3 (Family) A (Subfamily) 4(Form).

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8
Q

Which are the substances than inhibit Cyp 450?

A

[CRACK AMIGOS] Cimetidine, Ritonavir(protease inhibitor),Amiodarone, Ciprofloxacin, Ketoconazol, Acute alcohol abuse, Macrolides (except azithromycin), Isoniazid, Grapefruit juice, Omeprazole, Sulfonamides.

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9
Q

Which are the inducers from CYP-450?

A

[Kenyon Rides Shotgun in Barbie’s Girl Car]Phenytoin, Rifampin, St. John’s wort, Barbiturates, Griseofulvin and carbamazepine.

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10
Q

Which drugs inhibit the alcohol metabolism, and which is the enzyme inhibited?

A

Fomepizole: inhibits alcohol dehydrogenase.
Disulfiram: inhibits acetaldehyde dehydrogenase.

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11
Q

Which is the drug that you have to use when you want to know that your patient drank alcohol?

A

Disulfiram because made the acetaldehyde up and that induce Nausea, Vomiting, Headache and Hypotension.

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12
Q

Which are another drugs with Disulfiram-like reaction?

A

1)Metronidazole. 2)Certain cephalosporins. 3)Procarbazine. 4) 1st generation sulfonylureas.

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13
Q

Causes of acidosis?

A

[MUD PILES ]Methanol, Uremia, Diabetic ketoacidosis, Paraldehyde or phenformin, Iron tablets or INH, Lactic acidosis (and shock), Ethylene glycol and Salicylates.

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14
Q

What is the antidote for methanol intoxication?

A

Ethanol and Fomepizol.

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15
Q

What is Zero-order elimination?

A

Plasma concentration decrease linearly with time.

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16
Q

Which drugs are Zero-order elimination?

A

Phenytoin, Ethanol and Aspirin ( at high or toxic concentration).

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17
Q

What is First-order elimination?

A

Rate of elimination is directly proportional to the drug concentration. Constant fraction of drug eliminated per unit time.

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18
Q

Plasma concentration drug is 10 at the 0 hrs, 7.5 at the 1 hrs and 5 at the 2 hrs, at what hour it will be 0 plasma concentration, if is it Zero-order elimination?

A

4 hour, it decrease 2.5 plasma concentration per hour.

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19
Q

Plasma concentration drug is 10 at the 0 hrs, 5 at the 1hrs, 2.5 at the 2 hrs, if it is First-order elimination, what plasma concentration it will be at the 4 hour?

A

0.625 at the 4 hrs, because it eliminated 50% of the plasma concentration per hour.

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20
Q

What is PKA?

A

Acid Dissociation constant.

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21
Q

In which environments are trapped phenobarbital, methotrexate, TCAs and aspirin?

A

Those trapped in basic environments.

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22
Q

Which is the treat for aspirin overdose?

A

Bicarbonate, also for all weak acids substance.

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23
Q

In which environment amphetamines are trapped, and what is the treat for overdose?

A

Trapped in acidic environments and it is treat with Ammonium chloride.

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24
Q

What do you have to give to eliminate acids?

A

You have to give bases, and give acids to help eliminate bases.

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25
Q

Drug ends with -azole. What does it do and give an example.

A

Ergosterol synthesis inhibitor, Ketoconazole.

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26
Q

Drug ends with -bendazole. What does it do and give an example.

A

Antiparasitic/antihelmintic. Mebendazole.

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27
Q

Drug ends with -cillin. What does it do and give an example.

A

Peptidpglycan synthesis inhibitor. Ampicillin. Antimicrobial

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28
Q

Drug ends with -cycline. What does it do and give an example.

A

Protein synthesis inhibitor. Tetracycline. Antimicrobial.

29
Q

Drug ends with -ivir. What does it do and give an example.

A

Neuraminidase inhibitor. Oseltamivir. Antimicrobial

30
Q

Drug ends with -navir. What does it do and give an example.

A

Protease inhibitor. Ritonavir. Antimicrobial.

31
Q

Drug ends with -ovir. What does it do and give an example.

A

DNA polymerase inhibitor. Acyclovir. Antimicrobial.

32
Q

Drug ends with -thromycin. What does it do and give an example.

A

Macrolide antibiotic. Azithromycin. Antimicrobial.

33
Q

Drug ends with -ane. What does it do and give an example.

A

Inhalation general anesthetic. Halothane. CNS.

34
Q

Drug ends with -azine. What does it do and give an example.

A

Typical antipsychotic. Thioridazine. CNS

35
Q

Drug ends with -barbital. What does it do and give an example.

A

Barbiturate. Phenobarbital. CNS

36
Q

Drug ends with -caine. What does it do and give an example.

A

Local anesthetic. Lidocaine. CNS

37
Q

Drug ends with -etine. What does it do and give an example

A

SSRI. Fluoxetine. CNS

38
Q

Drug ends with -ipramine. What does it do and give an example.

A

TCA. Imipramine. CNS

39
Q

Drug ends with -triptyline. What does it do and give an example.

A

TCA. Amitriptyline. CNS

40
Q

Drug ends with -triptan. What does it do and give an example.

A

5-HT (1B/1D) agonist. Sumatriptan. CNS

41
Q

Drug ends with -zepam. What does it do and give an example.

A

Benzodiazepine. Diazepam. CNS

42
Q

Drug ends with -zolam. What does it do and give an example.

A

Benzodiazepine. Alprazolam. CNS

43
Q

Drug ends with -chol. What does it do and give an example.

A

Cholinergic agonist. Bethanechol/carbachol. Autonomic

44
Q

Drug ends with -curium. What does it do and give an example.

A

Nondepolarizing paralytic. Atracurium. autonomic.

45
Q

Drug ends with -curonium. What does it do and give an example.

A

Nondepolarizing paralytic. Vecuronium. Autonomic

46
Q

Drug ends with -olol. What does it do and give an example.

A

Beta blocker. Propranolol. Autonomic.

47
Q

Drug ends with -stigmine. What does it do and give an example.

A

AChE inhibitor. Neostigmine. Autonomic

48
Q

Drug ends with -terol. What does it do and give an example.

A

Beta 2 agonist. Albuterol. Autonomic

49
Q

Drug ends with -zosin. What does it do and give an example.

A

Alpha 1 antagonist. Prazosin. Autonomic

50
Q

Drug ends with -afil. What does it do and give an example.

A

PDE-5 inhibitor. Sidenafil. Cardiovascular

51
Q

Drug ends with -dipine. What does it do and give an example.

A

Dihydropyridine Calcium channel blockers (CCB). Amlodipine. Cardiovascular.

52
Q

Drug ends with -pril. What does it do and give an example.

A

ACE inhibitor. Captopril. Cardiovascular

53
Q

Drug ends with -sartan. What does it do and give an example.

A

Angiotensin II receptor blocker. Losartan. Cardiovascular

54
Q

Drug ends with -statin. What does it do and give an example.

A

MHG-CoA reductase inhibitor. Atorvastatin. Cardiovascular.

55
Q

Drug ends with -dronate. What does it do and give an example.

A

Biphosphonate. Alendronate.

56
Q

Drug ends with -glitazone. What does it do and give an example.

A

PPAR-gamma activator(peroxisome proliferator activated Receptor- Gamma). Rosiglitazone.

57
Q

Drug ends with -Prazole. What does it do and give an example.

A

Proton pump inhibitor (ppi). Omeprazole.

58
Q

Drug ends with -prost. What does it do and give an example.

A

Prostaglandin analog. Latanprost.

59
Q

Drug ends with -tidine. What does it do and give an example.

A

H2 antagonist. Cimetidine

60
Q

Drug ends with -tropin. What does it do and give an example.

A

Pituitary hormone. Somatotropin.

61
Q

Drug ends with -ximab. What does it do and give an example.

A

Chimeric monoclonal Ab. Basiliximab

62
Q

Drug ends with -zumab. What does it do and give an example.

A

Humanized monoclonal Ab. Daclizumab.

63
Q

Which are the beta and alpha blockers?

A

Carvedilol and Labetalol.

64
Q

Which hepatic phase of metabolism is lost by geriatric patients? Which phase is mediated by cytochrome p450?

A

Phase I for both answers

65
Q

Which medication overdose can be treated with bicarbonate ?

A

Weak acids (ex. Aspirin)

66
Q

Which medication can be treated with ammonium chloride?

A

Weak bases (ex. Amphetamines)

67
Q

What medication inhibits alcohol dehydrogenase ?

A

Fomepizole.

68
Q

Which medication inhibit acetaldehyde dehydrogenase ?

A

Disulfiram.

69
Q

Which phase include reduction, oxidation and hydrolysis as a reactions?

A

Phase I.