Pharmacology Flashcards
Acidic drugs, such as phenytoin, bind primary to which one of the following plasma proteins?
A. Alpha-fetoprotein (AFP)
B. Lipoprotein
C. Albumin
D. Alpha-acid gylcoprotein (AAG)
E. Gamma globulin
Albumin
The main drug-binding proteins in plasma are albumin, apha1-acid glycoprotein and lipoproteins.
Albumin binds drugs and ligands, reducing serum concentration of these compounds. An example is serum calcium, the free (ionised) fraction needs to be corrected for albumin.
Drugs that are important for albumin binding are warfarin, digoxin, NSAIDs and benzodiazepines
What is the mechanism of action of clopidogrel?
Selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation
RANKL is the target for which DMARD?
Denosumab
- Binding RANKL suppresses bone resorption and slows progression of bone erosions
Medications to avoid with tamoxifen?
Bupropion, fluoxetine - strong CYP2D6 inhibitors
- Thus decrease tamoxifen activation
Isosorbide mononitrate MOA
Improves myocardial O2 delivery via coronary vasodilation and β O2 demand via β preload > β ventricular wall stress
Needs nitrate-free interval 8-12 hrs to reduce tolerance
MOA sotolol
K channel blocker; may prolong QT interval
What does high hepatic extraction ratio mean?
High enzyme activity metabolising the drug - thus almost all drug is removed
Does loading dose influence time taken to reach steady state?
NO
- It brings the mean concentration of drug to higher concentration, meaning reaches therapeutic range sooner BUT does not influence time to SS
MOA of ciclosporin?
IL2 antagonist
Tacrolimus MOA?
IL2 antagonist; better immunosuppression but more nephrotoxic and worse BGL control
- Tacrolimus inhibits T-lymphocyte activationby binding to FKBP-12, an intracellular protein
Indication for dialysis in chronic lithium toxicity?
Lithium level >2.5 and CNS involvement
What does the BCG vaccine protect against?
BCG vaccine has a documented protective effect against meningitis and disseminated TB in children. It does not prevent primary infection and, more importantly, does not prevent reactivation of latent pulmonary infection, the principal source of bacillary spread in the community
Rifampicin inducer or inhibitor?
RifampicINDUCER
MOA metaclopramide?
D2 antagonist
- CTZ in medulla oblongata
Medications which cause B12 deficiency
Alcohol, metformin, PPI, colchicine, phenytoin