Drugs Flashcards
What is the active metabolite of azathioprine?
6-mercaptopurine (6MP), and endpoint active metabolite is thioguanine if it goes through the HPRT pathway (the bad one)
Generic name for Imuran
Azathioprine
Purine analogue, blocks purine biosynthesis
Imuran (Azathioprine)
And also Cellcept is one as well
Which phase of the cell cycle is blocked by azathioprine?
S phase
Why do you check a TMPT on a patient you are about to start on Imuran?
Before you start someone on Imuran (Azathioprine), you should check a TMPT level because if they have a hereditary deficiency in the enzyme then the drug will be metabolized down the HPRT pathway which gives the person bone marrow suppression= bad
What drug do you not want someone to be on while they are on imuran?
Allopurinol (inhibits the TMPT and XO pathway)
Which enzyme does Cellcept inhibit?
Inosine monophosphate dehydrogenase (IMPDH)
How does Cellcept treat things?
Inhibits purine synthesis of T and B cells in particular, because these cells do NOT HAVE A PURINE SALVAGE PATHWAY!!!
Nitrogen mustard derivative which blocks DNA cell cycle synthesis
Cyclophosphamide
Name a few side effects of Cyclophosphamide
HEMORRHAGIC CYSTITIS
Azoospermia
Pulmonary fibrosis
Alopecia
What is cyclophosphamide (Cytoxan) the treatment of choice for?
Wegeners granulomatosis
What is the drug of choice to treat Wegeners?
Cyclophosphamide
What dose Cyclosporine inhibit?
T cell synthesis
How does cyclosporine work?
Inhibits cyclophilin - which blocks calcineurin - which decreases NFAT - which decreases IL-2
Gingival hyperplasia
Cyclosporine
Which organ do you watch out for when prescribing cyclosporine?
Kidneys! (Nephrotoxic)
Which drug is metabolized by Cytochrome P450 3A4
Cyclosporine
What cytochrome is Cyclosporine metabolized by?
Cytochrome P450 3A4
Name 4 drugs that will increase renal toxicity risk of Cyclosporine
NSAIDS
Aminoglycosides
Vancomycin
Amphotericin B
Name 4 Cytochrome p450 inducers?
Carbamazepine
Phenytoin
Phenobarbital
Rifampin
What HTN med do you give if you get Cyclosporine induced HTN?
Israpidine
What is the maximum amt of time you can be on Cyclosporine?
One year
Max Cyclosporine dose per day
5mg/kg
What do you use Thalidomine to treat?
Erythema nodosum leprosum
What does Imiquimod bind?
TLR-7
Thymidyline Kinase
The enzyme that acyclovir uses to work
What enzyme does acyclovir use to work?
Thymidyline kinase
What drug do you use to treat scabies in pregnant women
Precipitated sulfur
How does permethrin work?
Blocks sodium channels, paralyzing the mite
How does ivermectin work?
Blocks chloride channels, paralyzing the parasite
What enzyme level should you check on a person you are about to start on Imuran?
TMPT (because if they are deficient, then too much drug will be shuttled down the main pathway-HPRT)
What is the active metabolite of azathioprine?
6-MP
What enzyme converts 6-MP to 6-Thioguanine?
HPRT
*TPMT is the one that you check because if its too low the pathway goes too much down the HPRT
What is the endpoint of the azathioprine pathway (the end product?)
6-Thioguanine
What two things should you check for before starting someone on imuran?
Imuran(azathioprine) - you should check TMPT levels, and also make sure they are not on allopurinol
Name two purine synthesis inhibitors
Cellcept and Imuran
Which drug performs which action? (Cellcept vs Imuran)
- Inhibits de novo purine synthesis
- Inhibits S-phase specific purine synthesis
- Inhibits de novo purine synthesis = Cellcept
2. Inhibits S phase specific purine synthesis = Imuran
Why do you get nausea in Cellcept?
Because the drug is reacted by the epidermis and also the GI tract
Name the two most severe side effects of Cellcept
Progressive multifocal leukoencephalopathy &
Pure red cell aplasia
What is the active metabolite of cellcept
Mycophenolic acid
How is Cellcept excreted?
Kidneys
Which is cellcept: nephrotoxic or hepatotoxic?
Neither!
Name the enzyme MTX inhibits
Dihydrofolate reductase (DHFR)
Treat liver toxicity from MTX with?
Leucovorin
Name the molecule Cyclosporine inhibits
Cyclophillin. (Cyclophillin activates calcineurin in the presence of calcium and calmodulin)
Name some side effects of Cyclosporine
Gingival hyperplasia
Uric acid
Nephrotoxicity
Reversible hypertension
What vital sign should you check regularly in a patient on cyclosporine?
BP (bc cyclosporine can cause reversible HTN)
Side effect of hydroxyurea
Leg ulcers
Stelara inhibits which molecules?
IL-12/IL-23
Which subunit of the IL12/23 molecules does Stelara inhibit?
P40 subunit
What drug is a PDE4 small molecule inhibitor?
Otezla
Name Otezla’s mechanism of action
PDE4 inhibitor
Name Xeljanz mechanism of action
JAK inhibitor
Side effect of cosyntyx
Nasopharyngitis
Which medication used to treat SLE,DM ect can cause blue-grey nail dispigmentation
Hydroxychlororquine (Plaquenil)
Name Plaquenil’s mechanism of action
Intercalates into DNA
What lab do you need to test before starting Plaquenil?
G6PD deficiency (And also should get a baseline eye exam)
Which eye findings in Plaquenil are reversible and which are not?
Visual field changes are reversible (premaculopathy)
Bull’s eye pigment retinopathy is not
Which antimalarial has no risk of retinopathy?
Quinacrine
What is a side effect of Quinacrine?
Yellow pigmentation of the skin
Which anti-malarial has the highest risk of G6PD hemolysis?
Primaquine
Mechanism of action of Rituxan
Monoclonal Ab, anti-CD20 (destroys B cells)
Common side effect of intralesional Bleomycin
Raynauds
Most common general cause of Fixed Drug Eruption
Tetracycline
Most common cause of non-pigmented fixed drug eruption
Psuedophed
Most common cause of fixed drug eruption in children
Bactrim
Which drug causes a sun exposed blue-grey dispigmentation
Amiodarone
Where does minocycline cause a blue grey dispigmentation?
On the legs
Which drug causes a blue-grey dispigmentation in the sclera, teeth, nailbeds and tibia?
Quinacrine
Cyclosporine metabolized by what enzyme
CYP3A (so don’t give itraconazole or erythromycin, or fluconazole or ketoconazole)
Half life of isotretinoin
20 hours
Side effect of foscarnet
Penile erosions
What drugs create gynecomastia?
*Some drugs cause awesome knockers
Spironolactone Digitalis Cimetidine Alcohol Ketoconazole
Are the inhibitors of 14-alpha-demethylase fungistatic or fungicidal?
Fungistatic
What two drugs cause inhibition of 14-alpha-demethylase?
Ketoconazole
Itraconazole
Which antifungal causes visual disturbances
Voriconazole
Which antifungals are CYT-p450 inhibitors?
Fluconazole
Voriconazole
&also ketoconazole btw
What antifungal is fungicidal?
Terbinafine (Lamisil)
Which two -azoles require an acidic environment for absorption?
Itraconazole and ketoconazole
Bad side effect of oral ketoconazole?
Fulminant hepititis
Which oral anti-fungal can cause fulminant hepatitis?
Ketoconazole *why they dont use it any longer orally
What enzyme does terbinafine inhibit?
Squalene epoxidase (first step of ergosterol synthesis)