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)
Which common antifungal DOES NOT inhibit cyp p450?
Terbinafine
What pregnancy category is terbinafine?
Category B
What side effect/autoimmune disease does terbinafine sometimes cause?
Drug induced LE
Which antifungal is at risk for causing drug induced LE?
Terbinafine
& griseofulvin
Which antifungal inhibits the first step of egrosterol synthesis?
Terbinafine! (Inhibits squalene epoxidase)
What enzyme mediates the first step of ergosterol synthesis?
Squalene epoxidase
Which antifungal disrupts microtubule formation?
Griseofulvin
Which antifungal is a cytochrome p450 INDUCER?
Griseofulvin
Which antiviral can cause TTP/HUS in HIV and transplant patients?
Valacyclovir
What is a bad side effect of using high doses of Valacyclovir in HIV or transplant patients?
TTP/HUS
What is the prodrug of acyclovir
Valacyclovir
Side effect of foscarnet
Penile erosions
Side effect:penile erosions
Foscarnet
Treatment for resistant HSV if failed acyclovir
Foscarnet
Why does foscarnet work when acyclovir doesnt?
Foscarnet does not require phosphorylation by viral thymidylate kinase like acyclovir does
What do you use if HSV is resistant to gancyclovir AND Foscarnet?
IV Cidofidir
Why does IV Cidofovir work when gancyclovir and foscarnet wont?
It acts completely INDEPENDANT of thymidylate kinase
Which antiviral works completely independant of thymidylate kinase?
Cidofivir
Which HIV medication causes melanonychia?
Zidovudine
Side effect of zidovudine?
Melanonychia
Which HIV medication can give a fatal hypersensitivity reaction?
Abacivir
Side effect of the protease inhibitor HIV meds
Periungal pyogenic granulomas
Which HIV med causes periungal pyogenic granulomas
The protease inhibitors (Indinavir, Ritonavir, Lopinavir)
Lice medication which is contraindicated if you are allergic to crysanthemums
Pyrethrin
How does Permethrin kill lice and scabies?
Disables the nerve cell Na transport channels
Which drug disables parasites sodium transport channels
Permethrin
Which antiparasitic disables:
Sodium channels?
Chloride channels?
Sodium channels - Permethrin
Chloride channels - Ivermectin
Name three diseases you use Ivermectin to treat?
Strongyloides
Onchocerciasis
Norwegian Scabies
Flammable anti-parasite drug
Malathion
Which anti-parasite medication blocks neural transmission by interfering wtih GABA
Lindane (used for scabies)
Which anti-parasitic carries an increased risk for seizures
Lindane (used for scabies, blocks GABA)
What do you use to treat cutaneous larva migrans?
Thiabendazole/Albendazole
What enzyme does Thiabendazole/Albendazole inhibit?
Fumarate reductase
Which antparasitic inhibits fumarate reductase
Thiabendazole,
*used to treat cutaneous larva migrans
Side effects of thiabendazole/albendazole
Dizziness, drowsiness, jaundice
Side effect of pentavalent antimonial (sodium stibogluconate, meglumine, antimoniate)
Prolonged QT interval
What do you use Pentamidine to treat?
Trypanosomiasis and leishmaniasis
What do you use DEC to treat?
Filariasis, onchocerciasis
Which cholesterol med reduces triglycerides the best?
Gemfibrozil
Hydrochlorothiazides known to cause what kind of reaction
Lichenoid eruption
Serum sickness is a side effect of which cephalosporin antibiotic?
Cefaclor
Can you use doxycycline in renal failure patient?
Yes, because it is excreted in the GI tract
Which part of the mouth does each medication stain?
-tetracycline
Vs
-minocycline
Tetracycline - stains the gingival 1/3
Minocycline - stains the mid-portion on the teeth
Which ribosomal subunit do the tetracyclines bind?
30s subunit
Which type of antibiotics bind the 30s subunit?
Tetracyclines
Which tetracycline is the most phototoxic?
Demeclocycline
Which antibiotic inhibits DNA-dependent RNA polymerase?
Rifampin
Which antibiotic is proven to decrease OCP efficacy?
Rifampin
Name two types of antibiotics which inhibit the 30s subunit
Tetracyclines
Aminoglycosides
Sulfonamides inhibit what enzyme?
Dihydropteroate synthetase
Name some antibiotics that bind the 50s ribosomal subunit?
Macrolides (Erythromycin)
Clindamycin
(*Tetracyclines and amminoglycosides bind the 30s subunit)
Treatment for CARP
Minocycline
Which antibiotic inhibits DNA gyrase
Fluoroquinolones
Side effect: acral erythema (erythrodysesthesia)
Doxyrubicin
5-FU
Cytarabine
MTX
*Vs bleomycin which causes acral sclerosis
Acral sclerosis
Bleomycin
*Bleomycin also causes Raynauds
Which antifungal can cause AGEP?
Terbinafine
Name some drugs that can cause AGEP
Beta lactam antibiotics (pinicillin) Macrolides (erythromycin) Terbinafine Calcium channel blocks (diltiazim) Chloriquine
Side effect: autoimmune hepatitis
Minocycline
What serious systemic side effect can minocycline cause?
Autoimmune hepatitis
Side effect: dermatomyositis-like eruption
Hydroxyurea
Eccrine squamous syringometaplasia
Cytarabine
Paclitaxel
A patient being treated with cytaribine and paclitaxel develops erythematous macules and papules in the axilla and on the hands. What side effect could this most likely be?
Eccrine squamous syringometaplasia
Drugs that cause Erythema Nodosum
OCPs
NSAIDS
Antibiotics (sulfonamides and tetracyclines)
Side effect: Extravasation reaction
Doxyrubicin
Side effect: flag sign
MTX
Side effect: gingival hyperplasia
Phenytoin
Cyclosporine
CCBs
Side effect: violetbrown/blue pigmentation of skin
Clofazimine
In which minocycline dyspigmentation reaction is iron not deposited into the skin?
Type III
Type I - pigment within scars (with iron deposition)
Type II - pigment on shins (with iron deposition)
Type III- pigment in sunexposed areas
Side effect: hypertrichosis
Cyclosporine
Phenytoin
Minoxidil
Side effect: inflamed SCCs
Fludaribine
Side effect: Inflamed SKs
Cytarabine
Which medication will cause a flare-up of inflamed seborrheic keratosis
Cytaribine
Side effect: leg ulcers
Hydroxyurea
Side effects of Hydroxyurea
Dermatomyositis-like eruption
Leg ulcers
Hydroxyurea inhibits what enzyme
Ribonucleotide reductase (inhibits DNA synthesis, S phase specific)
Side effect: leukocytoclastic vasculitis
Beta-lactam antibiotics (Penicillin)
Side effect: Lichenoid eruption
HCTZ
Beta-blockers
Quinidine
Which antimalarial causes a lichenoid-like eruption?
Quinidine
What is the most common cause of Linear IgA bullous dermatosis
Vancomycin
Side effect: flagellate hyperpigmentation
Bleomycin
Side effect: supravenous serpentine hyperpigmentation
5-FU
Side effect: sun exposed hyperpigmentation
MTX
5-FU
Daunorubicin
Side effect: hyperpigmentation of occluded areas
Thiotepa
Drugs causing:
SLE
Vs
SCLE
SLE: Hydralizine, procainimide, isoniazid, minocycline, phytanic, penicillamine
SCLE: Hydrochlorothiazide *most common), griseofulvin, terbinafine, CCBs
Most common cause of drug-induced SCLE
HCTZ
Name some causes of SCLE
HCTZ, Terbinafine, Griseofulvin
CCBs
Anticonvulsant hypersensitivity syndrome results from a defect in what enzyme
Epoxide hydroxylase
Antiparasitic which is an organophosphate cholinesterase inhibitor
Malathion
Side effect: melanonychia
Zidovudine (HIV med)
Side effect: mucositis
Daunorubicin Cyclophosphamide Doxorubicin MTX 5-FU
Neutrophilic eccrine hiddradentitis
Cytarabine
Side effect: onycholysis (non-photo)
Captopril
Retinoids
Chemo drugs: Paclitaxel, etopiside
Side effect: photo-onycholysis
Tetracyclines: doxycycline
OCPs
Flouroquinolones: Cipro
Psoralen
Side effect: pemphigus vulgaris
Captopril
Penacillamine
Side effect: pseudoporphyria
NSAIDS Furosemide HCTZ TCNs (doxycycline) Sulfonamides Isotretinoin Nalidixic acid
Side effect: induction or worsening of psoriasis
Terbinafine NSAIDS Captopril (ACE-I) Beta-blockers Lithium Antimalarials
Side effect: pulmonary fibrosis
MTX Bleomycin Amiodarone Penicillamine Gold Busulfan
Side effect: radiation recall
MTX
Actinomycetes-D
Doxorubicin, a ton of cancer drugs
Side effect: Raynaud’s phenomenon
Combo of bleomycin and vinblastine
Side effect: sweets
GCSF*
TMP-SMZ
Carbamazepine
Side effect: TEN
Allopurinol PCNs Anticonvulsants (carbamazepine, lamotigene, pheytoin) Sulfa drugs NSAIDS
Cytochrome P450 INDUCERS
Pretty Please Can I Rent Real Props for St Johns Only Gathering
Phenobarbital Phenytoin Carbamazepine Isoniazid Rifampin Ritonavir Propranolol St Johns Wart Omeprazole Griseofulvin
Which cell cycle specific phase does Bleomycin affect?
M and G2 phase specific - damages DNA by direct binding
Which chemotherapy drug damages DNA at M and G2 specific cell cycle phase?
Bleomycin
What is the Wolff-Chaikoff effect?
The inhibition of thyroid hormone synthesis when a patient is given Potassium Iodide
What side effect do you need to watch out for when giving Potassium Iodide?
Wolff-Chaikoff effect: inhibits thyroid hormone synthesis
What do you use to treat Sporotrichosis?
Potassium Iodide
What lab do you need to check one month after giving someone potassium iodide?
TSH
What is a contraindication of alendronate or other bisphosphonates?
Pregnancy
Which two antifungals should you not give to someone who is taking an antiacid and why?
Itraconazole and Ketoconazole
*because they both require an acidic environment to work, and they are both metabolized by the same enzyme (14-alpha-demethylase)
What enzyme do sulfonamide antibiotics inhibit?
Dihydopterase synthetase
Which retinoid has a risk of drug induced hypothyroidism
Bexarotene
Allopurinol blocks which enzyme in the azathioprine metabolic pathway?
XO (xanthene oxidase). *different from the genetically inherited TMPT deficiency
Most common drug to cause linear IgA
Vancomycin
Drug causing bullous pemphigoid
Furosemide
Name two drugs commonly causing pemphigus
Captopril
Penacillamine
Drug causing pseudoporphyria
Naproxen
Most common drug causing AGEP
B-lactams
Most common drug causing FDE on the penis
Sulfonamides
Name three common drugs causing phototoxic reactions
Tetracyclines
Quinolones
Psoralen
Drug causing palmoplantar erythrodysesthesia (Acral variant of toxic erythema of chemotherapy)
Cytaribine
Drug causing cicatricial pemphigoid
Clonidine
Most common class of medications to cause drug eruptions
Aminopenicillines > anticonvulsants >TMP/SMX > NSAIDS
Most common drug to cause drug reaction in HIV patients
Bactrim (TMP/SMX) - drug rash occurs in 40% of patients!
*vs the regular population, penicillins are the most common cause of drug reactions over bactrim
Time lag for ACE-I to develop lichenoid drug
How about quinacrine?
ACE-I - 6 months
Quinacrine - 6 weeks