Pharm/tox Flashcards
Which of the following is not associated with photosensitivity?
1) CBZ
2) Amiodarone
3) Lithium
4) TMP-SMX
5) Captopril
- Lithium
Photosensitivity drugs (top 10)
Doxycycline Hydrochlorothiazide Amiodarone Piroxicam Chlorpromazine Co-trimoxazole Captopril Enalapril Bendroflumethiazide Carbamazepine
SICK FACES?
CRAP GPs?
SICK FACES = CYP3A4 inhibitors
SSRIs Isoniazid CCBs (verapamil,diltiazem) Ketoconazole Fluconazole, metronidazole Amiodarone, allopurinol, ACUTE alcohol, antiretrovirals Clarithromycin Erythromycin Sodium valproate, sulfonamide
+ grapefruit juice
CRAP GPs = CYP3A4 inducers
Chronic ETOH
Rifampicin
Anti-epileptics (CBZ)
Phenytoin
Griseolfulvin
Phenobarituate
Smoking/St Johns wort
What is the equivalent of the following to 10mg PO morphine:
- endone
- S/C morphine
- hydromorphone PO and s/c
10mg morphine PO =
3mg morphine subcut (3)
7mg endone PO (1.5)
2mg hydromorphone PO (5)
Hydromorphone 10mg subcut to PO?
Morphine equivalent?
10mg subcut = 30mg oral (3)
30mg hydromorph PO = 150 PO morphine (5)
Equation for drug clearance
clearance = (Vd x 0.7)/half life
amiodarone increases cyclosporine concentrations via which mechanism?
PGP inhibition
Name 3 drugs which follow zero order kinetics
Alcohol
Phenytoin
Aspirin/salicylates
What is the active isomer of Warfarin?
S-warfarin (super warfarin!)
A patient is given 320mg loading dose of a medication. The peak serum concentration is 20mg. What is the Vd?
Vd = loading/peak concentration
320/20 = 16L
Equation for loading dose
Loading dose = Vd x target plasma concentration.
Difference between a non-competitive and competitive antagonist
Competitive antagonist
- Reversible binding. Maximum effect CAN be reached with higher dose of agonist (curve shifts right)
Non-competitive antagonist
- Non-reversible binding. Maximum effect CAN-NOT be achieved with higher dose of agonist (curve shifts down)
What is tachyphylaxis
Phenomenon of rapid decrease in the response to a drug due to previous (long term) exposure to that drug (i.e. amphetamines)
Indications for a liver transplant in panadol overdose
Acidosis (ph 7.3) Raised lactate (>3.0 with acidosis, >3.5 without) Coagulopathy (raised INR) + encephalopathy + AKI (creat >300)
Which class(es) of diabetic medications are associated with pancreatitis?
GLP1 agonists
DPP4 inhibitors
Which enzyme is involved in the metabolism of clopidogrel?
What is it’s effect on clopidogrel efficacy?
CYP2C19
Metabolizes clopidogrel to it’s active compound - therefore inhibiting CYP2C19 actually DECREASES clopidogrel’s efficacy
Against which receptors does norepinephrine have an agonist effect?
alpha1 and alpha 2
beta 1
Which medication classes are associated with jaw osteonecrosis
Antiresorptives* - RANK ligand inhibitors (denosumab), bisphosphonates
VEGF inhibitors - Mabs (i.e. bevacizumab, , TKIs (i.e. Sunitinib, lenvatinib)
*more common in cancer patients (high doses, immunosupressed)
Treatment for aspirin overdose
Urinary alkalization OR hemodialysis if indicated (i.e. severe AKI/CKD and can’t clear)
Charcoal if present within 2 hours
Drugs associated with crystal nephropathy
Acyclovir Sulfonamide antibiotics (i.e. TMP, bactrim) Ethylene glycol Mega dose vitamin C MTX Protease inhibitors “-navirs”
Which of the following has the greatest influence on steady state drug level? A. Clearance B. Elimination C. Half-life D. Volume of distribution E. Protein bounding
clearance
A drug has a fraction excreted unchanged of 0.1 and a total body clearance of 50L/hr. Liver blood flow is 90/L.
What is the maximum bioavailability of the drug?
A. 40%
B. 70%
C. 90%
D. 50%
D - 50%
Biovailability = 1 - HER
HER = total hepatic clearance/total liver blood flow.
Renal clearance 10%, therefore hepatic clearance 90%
90 + 10 = 50L (total body clearance)
Therefore 90% x 50L –> 45L/hr (hepatic clearance)
Liver blood flow = 90
45/90 = 50% therefore HER = 50%
100 - 50% = 50%
Which P2Y12 receptor antagonist irreversbly binds the receptor?
Ticagrelor (therefore short half life and TWICE daily dosing)
Prasugrel and clopidogrel = irreversible
binding
Name the receptor for each anti-emetic:
- palonosetron
- cyclizine
- aprepitant
- olanzapine
- metoclopramide
Palonosetron = 5HT3 Cyclizine = 5HT1 Aprepitant = NK1 receptor Olanzapine = 5HT2 + dopamine Metoclopramide = D2 + 5HT3
Statins that undergo CYP3A4 metabolism
atorvastatin
simvastatin
Metabolism of isoniazid
Clinical relevance?
Primarily metabolized by acetylation and dehydrazination
Rate of acetylation is genetically determined.
- 50% are “slow acetylators” and 50% “rapid acetylators” (more common in asians)
slow acetylation = higher blood levels, more toxicity (i..e HEPATITIS)
rapid acetylation = lower blood levels, less efficacy