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
Drug ends with -cycline. What does it do and give an example.
Protein synthesis inhibitor. Tetracycline. Antimicrobial.
Drug ends with -ivir. What does it do and give an example.
Neuraminidase inhibitor. Oseltamivir. Antimicrobial
Drug ends with -navir. What does it do and give an example.
Protease inhibitor. Ritonavir. Antimicrobial.
Drug ends with -ovir. What does it do and give an example.
DNA polymerase inhibitor. Acyclovir. Antimicrobial.
Drug ends with -thromycin. What does it do and give an example.
Macrolide antibiotic. Azithromycin. Antimicrobial.
Drug ends with -ane. What does it do and give an example.
Inhalation general anesthetic. Halothane. CNS.
Drug ends with -azine. What does it do and give an example.
Typical antipsychotic. Thioridazine. CNS
Drug ends with -barbital. What does it do and give an example.
Barbiturate. Phenobarbital. CNS
Drug ends with -caine. What does it do and give an example.
Local anesthetic. Lidocaine. CNS
Drug ends with -etine. What does it do and give an example
SSRI. Fluoxetine. CNS
Drug ends with -ipramine. What does it do and give an example.
TCA. Imipramine. CNS
Drug ends with -triptyline. What does it do and give an example.
TCA. Amitriptyline. CNS
Drug ends with -triptan. What does it do and give an example.
5-HT (1B/1D) agonist. Sumatriptan. CNS
Drug ends with -zepam. What does it do and give an example.
Benzodiazepine. Diazepam. CNS
Drug ends with -zolam. What does it do and give an example.
Benzodiazepine. Alprazolam. CNS
Drug ends with -chol. What does it do and give an example.
Cholinergic agonist. Bethanechol/carbachol. Autonomic
Drug ends with -curium. What does it do and give an example.
Nondepolarizing paralytic. Atracurium. autonomic.
Drug ends with -curonium. What does it do and give an example.
Nondepolarizing paralytic. Vecuronium. Autonomic
Drug ends with -olol. What does it do and give an example.
Beta blocker. Propranolol. Autonomic.
Drug ends with -stigmine. What does it do and give an example.
AChE inhibitor. Neostigmine. Autonomic
Drug ends with -terol. What does it do and give an example.
Beta 2 agonist. Albuterol. Autonomic
Drug ends with -zosin. What does it do and give an example.
Alpha 1 antagonist. Prazosin. Autonomic
Drug ends with -afil. What does it do and give an example.
PDE-5 inhibitor. Sidenafil. Cardiovascular
Drug ends with -dipine. What does it do and give an example.
Dihydropyridine Calcium channel blockers (CCB). Amlodipine. Cardiovascular.
Drug ends with -pril. What does it do and give an example.
ACE inhibitor. Captopril. Cardiovascular
Drug ends with -sartan. What does it do and give an example.
Angiotensin II receptor blocker. Losartan. Cardiovascular
Drug ends with -statin. What does it do and give an example.
MHG-CoA reductase inhibitor. Atorvastatin. Cardiovascular.
Drug ends with -dronate. What does it do and give an example.
Biphosphonate. Alendronate.
Drug ends with -glitazone. What does it do and give an example.
PPAR-gamma activator(peroxisome proliferator activated Receptor- Gamma). Rosiglitazone.
Drug ends with -Prazole. What does it do and give an example.
Proton pump inhibitor (ppi). Omeprazole.
Drug ends with -prost. What does it do and give an example.
Prostaglandin analog. Latanprost.
Drug ends with -tidine. What does it do and give an example.
H2 antagonist. Cimetidine
Drug ends with -tropin. What does it do and give an example.
Pituitary hormone. Somatotropin.
Drug ends with -ximab. What does it do and give an example.
Chimeric monoclonal Ab. Basiliximab
Drug ends with -zumab. What does it do and give an example.
Humanized monoclonal Ab. Daclizumab.
Which are the beta and alpha blockers?
Carvedilol and Labetalol.
Which hepatic phase of metabolism is lost by geriatric patients? Which phase is mediated by cytochrome p450?
Phase I for both answers
Which medication overdose can be treated with bicarbonate ?
Weak acids (ex. Aspirin)
Which medication can be treated with ammonium chloride?
Weak bases (ex. Amphetamines)
What medication inhibits alcohol dehydrogenase ?
Fomepizole.
Which medication inhibit acetaldehyde dehydrogenase ?
Disulfiram.
Which phase include reduction, oxidation and hydrolysis as a reactions?
Phase I.
