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60 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What are the Phase I reactions in drug metabolism? |
HOR Hydrolysis Oxidation Reduction
(with cytochrome 450) |
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What characteristics do phase I metabolites have? |
Slightly polar Water soluble Active |
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What goes first? Phase I or II? |
they can go in EITHER order or EITHER OR |
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What are the phase II reactions in drug metabolism? |
GAS Glucuronidation Acetylation Sulfation Methylation (all conjugation reactions) |
Geriatric patients have GAS |
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What phase do geriatric patients lose in drug metabolism? |
Both, but they can lose phase I first. |
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What characteristics do phase II metabolites have? |
Very polar Inactive (Renally excreted) |
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People who are slow acetylators... |
Have greater side effects from certain drugs because their is a decreased metabolism. BUILT-UP substance, higher risk of toxicity. |
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What cytochrome P450 metabolizes 50% of all drug reactions? |
CYP3A4 |
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If you administer 2 drugs that are metabolized by the same cytochrome P450, what might happen? |
longer for both drugs to be inactivated, increased plasma levels or prolonged action of one or both drugs |
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What substances inhibit cytochrome p450? |
CRACK AMIGOS: Cimentidine, Ritonavir, Amiodarone, Ciprofloxacin, Ketoconazole, Acute alcohol use, Macrolides, Isoniazid, Grapefuit juice, Omeprazol, Sulfonamides. |
CRACK AMIGOS: inhibit yourself from it ;) |
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What substances induce cytochrome p450? |
Guinness, Coronas and PBRs induce Chronic Alcoholism
Griseofulvin, Carbamazepin, Phenytoin, Barbituates, Rifampin, St. Johns wort, Chronic alcoholism |
Guinness, Coronas and PBRs induce chronic alcoholism |
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What are the 2 key enzymes responsible in ethanol metabolism? |
Ethahol->Alchohol dehydrogenase->Acetaldehyde->Acetaldehyde dehydrogenase->Acetate
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What drug inhibits the enzyme alcohol dehydrogenase? |
Fomepizole - It can be used in intoxication with methanol and ethylene glycol Ethanol - Competes for attention from enzyme |
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What SE does methanol intoxication produce? |
Formaldehyde, the toxic metabolite, causes SE of acidosis, retinal damage, blindness |
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What SE does ethylene glycol intoxication produce? |
Oxalic acid, the toxic metabolite, causes SE of acidosis, kidney problems (bc of crystal depsits), CNS problems, heart/lung toxicity? |
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In what cases might you see methanol and ethylene glycol intoxication? |
Methanol is used by some dumbasses to get drunk or to commit suicide. Whereas ethylene glycol is sweet and ingested by kids and animals. |
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What drug inhibits the enzyme acetaldehyde dehydrogenase? |
Disulfiram It is used in treatment for alcoholism by making acetaldehyde build up
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What SE does acetaldehyde accumulation produce? |
Flushing, sweating, headache, headache, nausea, vomiting, hypotension |
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What drugs cause disulfiram-like reaction? |
- Metronizadole - Certain cephalosporins - Procarbazine - 1st generation sulfonylureas |
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What is zero-order elimination? |
- Constant amount of drug eliminated per unit time (e.g. constant miligrams per hour) - Plasma concentration decreases linearly with time |
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What drugs are zero-order elimination? |
PEA: round like 0
Phenytoin Ethanol Aspirin |
PEA |
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What is first-order elimination? |
- Constant proportion (%) of drug is eliminated per unit of time (regarless the mg) - Plasma concentration decreases exponentially with time
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After a drug has been inactivated, what are the two routes of elimination? |
- Bile->feces - Renal->Urine |
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What characteristics do inactive drugs need to have in order to be cleared quickly by the kidney? |
They must be polar, hydrophilic, charged (ionized) species in order to get trapped in the urine. Neutral forms can be reabsorbed. |
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What is the acid dissociation constant? |
"pKa"
Is the pH at which the non-protonated form (A + B) = the amount of protonated form (HA or BH) |
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If pH < pKa, what will you expect to see? |
If pH is low (acidic) , and less than pKa, there will be more protonated form. |
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If pH > pKa, what will you expect to see? |
If pH is high (basic), and more than pKa, there will be more of the nonprotonated form. |
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What substances get trapped in the urine in basic enviroments? |
Weak acids: RCOO- + H+
Phenobartital, methotrexate, aspirin |
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What substances get trapped in the urine in acidic enviroments? |
Weak bases: NH3+
Amphetamines |
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How do you treat acid drug overdose? |
Bicarbonate |
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How do you treat basic drug overdose? |
Ammonium chloride |
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-ane |
An inhalatory general anesthetic drug like halothane, isoflurane, sevoflurane |
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-azine |
typical antipsychotic like thioridazine, chloropromazine |
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-etine |
A selective serotonin reuptake inhibitor like fluoxetine (Prozac), sertratine |
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-ipramine |
TCA like imipramine, clomipramine |
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-triptan |
serotonin agonst like sumatriptan, risatriptan (migraine tx) |
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-triptyline |
TCA like amitriptyline, nortriptyline |
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-zepam & -zolam |
benzodiazepines like diazepam, lorazepam, alprazolam, midazolam |
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-chol |
cholinergic agonists like bethancol (urinary retention, neurogenic ileum), carbachol (glaucoma) |
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-curium or curinium |
non-depolarizing paralytic like atracurium, becuronium |
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-stigmine |
AChE inhibitor like neostigmine (neurogenic ileum and retention), physostigmine (glaucoma), rivastigmine (alzheimer) |
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-zosin |
alfa-1 antagonist like prazosin, doxazosin (both are used to lower BP and control anxiety,panic) |
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-afil |
Phosphodiesterase inhibitor like sildenafir and tadalafil (viagra) |
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-dipine |
calcium channel blocker like amlodipine, nifedipine (tx HTN) |
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-pril |
ACE inhibitor like captopril, enalpril (tx HTN) |
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-sartan |
Angiotensin II receptor blocker like losartan, valsartan |
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-statin |
HMG-CoA reductase inh (lower cholesterol) like atorvastatin, simvastatin |
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-dronate |
Biphosphonate (prevents bone loss, used in osteoporosis tx) like alendronate, risedronate |
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-glitazone |
thiazolidinedione/PPAR-y activator (antidiabetic) like rosiglitazone, pioglitazone |
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-tidine |
H2 antagonist (blocks histamine on parietal cells and blocks acid secretion) like cimetidine, ranitidine |
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-tropin |
pituitary hormone like somatotropin, thryotropin |
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-operidol |
neuroleptic (mayor tranquilizers) like haloperidol and droperidol |
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-phylline |
methylxantine (COPD and asthma) like theophylline and aminophylline |
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-ximab |
chimeric monoclonal Ab like basiliximab, infliximab |
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-zumab |
humanized monoclonal Ab like daclizumab |
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-gliptin |
DDP-IV inhibitor (tx:DM2) like sitagliptin, saxagliptin |
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-mustine |
nitrosourea (brain tumors) like lomustustine |
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-azole |
Ergosterol synthesis inhibitor like ketoconazol and fluconazol |
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-cillin |
peptidogylcan synthesis inhibitor (penicillin antiobiotic) like ampicilin, amoxicillin |
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-cycline |
protein synthesis inhibitor like tetracycline, doxycycline |
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