Primer 21 - Drug Metabolism Flashcards
Which metabolites does yield from phase I?
1) Sightly polar. 2) Water-soluble. 3) Active.
Which are the reaction and metabolites yield from phase II?
Reactions (conjugation): Glucuronidation, Acetylation and Sulfation “GAS”.
Metabolites: Very polar and inactive.
Which is the phase that geriatric patients lose?
Phase I, Geriatric patients have GAS (phase II).
Which cytochrome performance phase I reactions?
Cytochrome P-450 in liver.
What kind of patients are more susceptibles for high side effects?
Patients who are slow acetylators have increase side effects from certain drugs because of decrease rate of metabolism.
What is happened when two drugs have the same metabolism by Cytochrome P-450?
Drug-drug interaction, one of them drugs going to increase in serum plasma levels or prolong the action.
What is the subfamily type of CYP3A4?
CYP (Cytochrome) 3 (Family) A (Subfamily) 4(Form).
Which are the substances than inhibit Cyp 450?
[CRACK AMIGOS] Cimetidine, Ritonavir(protease inhibitor),Amiodarone, Ciprofloxacin, Ketoconazol, Acute alcohol abuse, Macrolides (except azithromycin), Isoniazid, Grapefruit juice, Omeprazole, Sulfonamides.
Which are the inducers from CYP-450?
[Kenyon Rides Shotgun in Barbie’s Girl Car]Phenytoin, Rifampin, St. John’s wort, Barbiturates, Griseofulvin and carbamazepine.
Which drugs inhibit the alcohol metabolism, and which is the enzyme inhibited?
Fomepizole: inhibits alcohol dehydrogenase.
Disulfiram: inhibits acetaldehyde dehydrogenase.
Which is the drug that you have to use when you want to know that your patient drank alcohol?
Disulfiram because made the acetaldehyde up and that induce Nausea, Vomiting, Headache and Hypotension.
Which are another drugs with Disulfiram-like reaction?
1)Metronidazole. 2)Certain cephalosporins. 3)Procarbazine. 4) 1st generation sulfonylureas.
Causes of acidosis?
[MUD PILES ]Methanol, Uremia, Diabetic ketoacidosis, Paraldehyde or phenformin, Iron tablets or INH, Lactic acidosis (and shock), Ethylene glycol and Salicylates.
What is the antidote for methanol intoxication?
Ethanol and Fomepizol.
What is Zero-order elimination?
Plasma concentration decrease linearly with time.
Which drugs are Zero-order elimination?
Phenytoin, Ethanol and Aspirin ( at high or toxic concentration).
What is First-order elimination?
Rate of elimination is directly proportional to the drug concentration. Constant fraction of drug eliminated per unit time.
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?
4 hour, it decrease 2.5 plasma concentration per hour.
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?
0.625 at the 4 hrs, because it eliminated 50% of the plasma concentration per hour.
What is PKA?
Acid Dissociation constant.
In which environments are trapped phenobarbital, methotrexate, TCAs and aspirin?
Those trapped in basic environments.
Which is the treat for aspirin overdose?
Bicarbonate, also for all weak acids substance.
In which environment amphetamines are trapped, and what is the treat for overdose?
Trapped in acidic environments and it is treat with Ammonium chloride.
What do you have to give to eliminate acids?
You have to give bases, and give acids to help eliminate bases.
Drug ends with -azole. What does it do and give an example.
Ergosterol synthesis inhibitor, Ketoconazole.
Drug ends with -bendazole. What does it do and give an example.
Antiparasitic/antihelmintic. Mebendazole.
Drug ends with -cillin. What does it do and give an example.
Peptidpglycan synthesis inhibitor. Ampicillin. Antimicrobial