Pharma Flashcards
Short acting Frenzodiazepams TOM
Triazolam Oxazepam Midazolam
1st line for Pseudomonas
antipseudomonal PCN + amnoglycoside. Pip Tazo plus Genta. PP Pseudomonas is Pip Tazo.
Antibiotic requiring oxygen for uptake into host cell therefore not effective against anaerobes
aminoglycoside
synergistic antibiotics
Beta lactam plus aminoglycoside
Drugs that cause coronary vasospasm
Cocaine Sumatriptan Ergot alkaloid
Drugs that cause cutaneous flushing VANC
Vancomycin Adenosine Niacin Ca channel blocker
Drugs that cause dilated cardiomyopathy
Doxorubicin (adriamycin) Daunorubicin
Cause torsade de pointes
Class III (sotalol) and class Ia (quinidine) antiarrhythmics
Cause agranulocytosis
Clozapine Carbamazepine Colchicine Propylthiouracil Methimazole Dapsone
Cause aplastic anemia
Chloramphenicol Benzene NSAIDs PTU Methimazole
Direct Coombs test positive
Methodopa Penicillin
SE
Gray baby syndrome
Chloramphenicol
SE
Hemolysis in G6PD. IS PAIN
Isoniazid Sulfonamide Primaquine ASA Ibuprofen
Nitrofurantoin
SE
MegaloBLASTic anemia
Phenytoin Methotrexate Sulfa drugs
SE thrombotic complications
OCP
SE pulmonary fibrosis
Bleomycin Amiodarone Busulfan
SE
Acute cholestatic hepatitis , jaundice
Erythromycin
SE
Focal to massive hepatic necrosis
Halothane Amanita phylloides Valproic acid Acetaminophen
Hepatitis
Isoniazid
Pseudomembranous colitis cause
Ampicillin clindamycin
SE
Adrenocortical suppression
Withdrawal of steroids
SE
Gynecomastia
Some Drugs Create Awkward Knockers
Spirinolactone digitalis cimetidine alcohol ketoconazole
SE
Hot flashes
Tamoxifen clomiphene
SE
Hyperglycemia
Niacin , tacrolimus ,protease inhibitors, hctz, steroids
SE
Hypothyroidism
Lithium Amiodarone sulfonamide
Most vestibulotoxic aminoglycoside
Gentamicin.
SE
Aminoglycosides
Nephrotoxicity and ototoxicity.
Extra pyramidal effects of antipsychotics after 4 hours, 4 days, 4 weeks, 4 months?
4 hours Acute dystonia - involuntary spasm of facial muscles only
4 days Akinesia - Parkinson like
4 weeks Akathisia - feeling of restlessness
4 months Tardive dyskinesia - involuntary spasm of facial muscles plus trunk, extremities
Slow involuntary writhing movement of hands and feet seen in cerebral palsy or Huntingtons disease
Athetosis
Chemo for ESTROGEN + or PROGESTERONE + receptor breast Ca
Tamoxifen
Monoclonal antibody against human epidermal growth factor receptor 2
Transtuzumab or herceptin used in breast ca with HER2 over expression
Therapeutic antibody against CD 20 of B cell NHL
Rituximab
Therapeutic antibody against TNF alpha used in crohn’s ds, rheumatoid arthritis, psoriatic arthritis
Infliximab, adalimumab
Asthma drugs. Identify drug class Ipratropium vs Salmetrol vs albuterol
Ipratropium anti muscarinic. Competitively bucks muscarinic r
Salmetrol long acting beta 2 agonist works up to 12 hours
Albuterol short acting beta 2 agonist 3 to 6 hours
Therapeutic antibody vs VEGF used in macular degeneration and colon, breast or non small cell lung ca.
Bevacizumab or Ranibizumab
What is ABVD used for Hodgkin’s lymphoma ?
A adriamycin (doxorubicin). intercalates DNA
B bleomycin - SE pulmonary fibrosis. Induces DNA strand breaks
V vinblastine - inhibit micro tubule assembly (Metaphase)
D dacarbizine - alkylation agent
Blocks t type calcium channels used in absence with SE of SJS
Ethosuximide
MOA Valproic acid
Inc GABA in brain, inc na channel inactivation
Anti epileptic drugs that Increase Na channel inactivation
Phenytoin, carbamazepine
First line generalized tonic clonic seizure
Phenytoin, carbamazepine
First line partial simple or complex seizure
Carbamazepine
Status epileptics meds
Benzodiazepams (diazepam or lorazepam) and phenytoin
Moa phenobarbital
Inc GABA action
Irreversibly inhibits GABA
Vigabatrin
MOA Gabapentin
Inhibit Calcium channels
Topiramate MOA
Blocks Na channels and Inc GABA action
Chemo drugs acting on S phase
Antimetabolites: 5FU, methotrexate, mercaptopurine
Etoposide
Chemo drugs acting on G2 phase
Synthesis of components needed for mitosis
Etoposide
Bleomycin
Inhibit formation of pyrimidines
5FU, methotrexate
Inhibit formation of purines
Mercaptopurine
SE neural tube defect vs fetal hydantoin syndrome
neural tube defect : Valproic acid
fetal hydantoin syndrome: Phenytoin
Inhibits thymidylate synthase vs dihydrofolate reductase
thymidylate synthase inhibitor: 5FU
dihydrofolate reductase: methotrexate
Inhibits bacterial transpeptidase
Penicillin drug class
Most vestibulotoxic aminoglycoside
Gentamicin.
SE
Aminoglycosides
Nephrotoxicity and ototoxicity.
Extra pyramidal effects of antipsychotics after 4 hours, 4 days, 4 weeks, 4 months?
4 hours Acute dystonia - involuntary spasm of facial muscles only
4 days Akinesia - Parkinson like
4 weeks Akathisia - feeling of restlessness
4 months Tardive dyskinesia - involuntary spasm of facial muscles plus trunk, extremities
Slow involuntary writhing movement of hands and feet seen in cerebral palsy or Huntingtons disease
Athetosis
Chemo for ESTROGEN + or PROGESTERONE + receptor breast Ca
Tamoxifen
Monoclonal antibody against human epidermal growth factor receptor 2
Transtuzumab or herceptin used in breast ca with HER2 over expression
Therapeutic antibody against CD 20 of B cell NHL
Rituximab
Therapeutic antibody against TNF alpha used in crohn’s ds, rheumatoid arthritis, psoriatic arthritis
Infliximab, adalimumab
Asthma drugs. Identify drug class Ipratropium vs Salmetrol vs albuterol
Ipratropium anti muscarinic. Competitively bucks muscarinic r
Salmetrol long acting beta 2 agonist works up to 12 hours
Albuterol short acting beta 2 agonist 3 to 6 hours
Therapeutic antibody vs VEGF used in macular degeneration and colon, breast or non small cell lung ca.
Bevacizumab or Ranibizumab
What is ABVD used for Hodgkin’s lymphoma ?
A adriamycin (doxorubicin). intercalates DNA
B bleomycin - SE pulmonary fibrosis. Induces DNA strand breaks
V vinblastine - inhibit micro tubule assembly
D dacarbizine - alkylation agent
Blocks t type calcium channels used in absence with SE of SJS
Ethosuximide
MOA Valproic acid
Inc GABA in brain, inc na channel inactivation
Anti epileptic drugs that Increase Na channel inactivation
Phenytoin, carbamazepine
First line generalized tonic clonic seizure
Phenytoin, carbamazepine
First line partial simple or complex seizure
Carbamazepine
Status epileptics meds
Benzodiazepams (diazepam or lorazepam) and phenytoin
Moa phenobarbital
Inc GABA action
Irreversibly inhibits GABA
Vigabatrin
MOA Gabapentin
Inhibit Calcium channels
Topiramate MOA
Blocks Na channels and Inc GABA action
Chemo drugs acting on S phase
Antimetabolites: 5FU, methotrexate, mercaptopurine
Etoposide
Chemo drugs acting on G2 phase
Synthesis of components needed for mitosis
Etoposide
Bleomycin
Inhibit formation of pyrimidines
5FU, methotrexate
Inhibit formation of purines
Mercaptopurine
SE neural tube defect vs fetal hydantoin syndrome
neural tube defect : Valproic acid
fetal hydantoin syndrome: Phenytoin
Inhibits thymidylate synthase vs dihydrofolate reductase
thymidylate synthase inhibitor: 5FU
dihydrofolate reductase: methotrexate
Inhibits bacterial transpeptidase
Penicillin drug class
Most vestibulotoxic aminoglycoside
Gentamicin.
SE
Aminoglycosides
Nephrotoxicity and ototoxicity.
Extra pyramidal effects of antipsychotics after 4 hours, 4 days, 4 weeks, 4 months?
4 hours Acute dystonia - involuntary spasm of facial muscles only
4 days Akinesia - Parkinson like
4 weeks Akathisia - feeling of restlessness
4 months Tardive dyskinesia - involuntary spasm of facial muscles plus trunk, extremities
Slow involuntary writhing movement of hands and feet seen in cerebral palsy or Huntingtons disease
Athetosis
Chemo for ESTROGEN + or PROGESTERONE + receptor breast Ca
Tamoxifen
Monoclonal antibody against human epidermal growth factor receptor 2
Transtuzumab or herceptin used in breast ca with HER2 over expression
Therapeutic antibody against CD 20 of B cell NHL
Rituximab
Therapeutic antibody against TNF alpha used in crohn’s ds, rheumatoid arthritis, psoriatic arthritis
Infliximab, adalimumab
Asthma drugs. Identify drug class Ipratropium vs Salmetrol vs albuterol
Ipratropium anti muscarinic. Competitively bucks muscarinic r
Salmetrol long acting beta 2 agonist works up to 12 hours
Albuterol short acting beta 2 agonist 3 to 6 hours
Therapeutic antibody vs VEGF used in macular degeneration and colon, breast or non small cell lung ca.
Bevacizumab or Ranibizumab
What is ABVD used for Hodgkin’s lymphoma ?
A adriamycin (doxorubicin). intercalates DNA
B bleomycin - SE pulmonary fibrosis. Induces DNA strand breaks
V vinblastine - inhibit micro tubule assembly
D dacarbizine - alkylation agent
Blocks t type calcium channels used in absence with SE of SJS
Ethosuximide
MOA Valproic acid
Inc GABA in brain, inc na channel inactivation
Anti epileptic drugs that Increase Na channel inactivation
Phenytoin, carbamazepine
First line generalized tonic clonic seizure
Phenytoin, carbamazepine
First line partial simple or complex seizure
Carbamazepine
Status epileptics meds
Benzodiazepams (diazepam or lorazepam) and phenytoin
Moa phenobarbital
Inc GABA action
Irreversibly inhibits GABA
Vigabatrin
MOA Gabapentin
Inhibit Calcium channels
Topiramate MOA
Blocks Na channels and Inc GABA action
Chemo drugs acting on S phase
Antimetabolites: 5FU, methotrexate, mercaptopurine
Etoposide
Chemo drugs acting on G2 phase
Synthesis of components needed for mitosis
Etoposide
Bleomycin
Inhibit formation of pyrimidines
5FU, methotrexate
Inhibit formation of purines
Mercaptopurine
SE neural tube defect vs fetal hydantoin syndrome
neural tube defect : Valproic acid
fetal hydantoin syndrome: Phenytoin
Inhibits thymidylate synthase vs dihydrofolate reductase
thymidylate synthase inhibitor: 5FU
dihydrofolate reductase: methotrexate
Inhibits bacterial transpeptidase
Penicillin drug class
Medication for Alzheimer’s that inhibits cholinesterase ie indirect cholinomimetic.
Donepezil
Not a cure, slows down disease but does not alter course.
Multinucleated giant cells. After initial infection, travels in retrograde manner to DRG.
Enveloped ds DNA virus.
HSV
Tzank smear
CYP 450 Inhibitors
Quin V inhibited was SICK with RAGE
Quinidine V inhibited was Sulfonamides Isoniazid Cimetidine Ketoconazole Riot avid Amniodarone Grapefruit Erythromycin
CYP 450 Inducers
Momma Ethel Booba Phoned Refusing Smoked or Grilled Carp
Modafinil Ethanol Barbidurates Phenytoin aka phenobarbiedoll Rifampicin Smoking or St. John's wort Griseofulvin Carbamazepine
Bactericidal antibiotics
Very Finely Proficient At Murder
Vancomycin - binds D ala D ala Fluroquinolone - inhibits DNA gyrase PCN - bind transpeptidase Aminoglycoside - inhibits initiation complex , 30s Metronidazole -
Bacteriostatic antibiotics
BacteriostaTTECCS
Trimethoprim Tetracycline Erythromycin Clindamycin Chloramphenicol Sulfamethoxazole
Antifungal: disrupts membrane function
Amphotheracin B
Nystatin
Antifungal: disrupts cell wall synthesis
Caspofungin
Anidulfungin
Antifungal: disrupts ergosterol synthesis
Fluconazole
Itraconazole
Voriconazole
Antifungal: disrupts lanosterol synthesis
Terbinafine
Naftifine
SE of protease inhibitors “navir”s used in HIV tx
Lipodystrophy - fat redistribution
Hyperglycemia
GI intolerance, Nephropathy, Hematuria (indinavir)
Lopinavir, Atazanavir, Ritonavir, Indinavir, etc
Nucleoside reverse transcriptase inhibitors NRTI side effect.
Bone marrow suppression
Peripheral neuropathy
Anemia - zidovudine
Didanosine, lamivudine, abacavir, tenofovir, zidovudine formerly azt,
Effect of drug on body
PharmacoDynamics
Effect of body on the drug
Pharmacokinetics
of hours max for pralidoxime to work
6 to 8 hrs
Used like atropine for organophosphate poisoning
Used to alkalinize or acidify urine
alkalinize urine - make it Basic with Bicarbonate
acidify urine - make it Acidic with Ammonium chloride
Sublingual hypertensive meds pathway
Lingual vein -> IJV -> brachiocephalic or innominate vein -> SVC -> RA
Rectal route of meds partial first pass because
Superior rectal vain -> IMV -> portal system FIRST PASS
Middle rectal vein -> IIV -> IVC
Inferior rectal vein -> IPV -> IIV -> IVC
Best topical preparation
Ointment > foam > cream
Slowest drug route
Routes of administration
Significant first pass effect ?
Partially bypasses first pass effect ?
Completely bypasses first pass effect ?
Significant first pass effect ? Oral
Partially bypasses first pass effect ? Rectal
Completely bypasses first pass effect ? IV, IM, SC, SL, inhalation, topical, transdermal (systemic effect)
Soluble drugs are _____ & ________
Non ionized and non polar aka lipid soluble
Drugs that have zero order kinetics ie constant elimination rate over time / Linear
WHAT PET
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Note. NO Half life in zero order!!!
Dosage required to have 50% efficacy aka amount needed to produce a given effect.
Potency
Efficacy is the height of the curve, potency is concentration in x axis
Concentration required to bind 50% of receptors
Kd
High Kd, low affinity etc
Measures of potency
ED50 median effective
TD50 median toxic
LD50 median lethal
Agonist + competitive antagonist
Dec potency but same efficacy.
Lower Kmax, same Vmax
Shift to the right. You need more to obtain same effect in presence of competitive antagonist.
Agonist plus concompetitive antagonist
DECrease efficacy, with same potency.
Lower Vmax, same Kd
Idiosyncratic effect of allopurinol
Cataract
First order kinetics. Drugs metabolized 1, 2, 3 half life
1st half life 50%
2nd half life 75 %
3rd half life 87.5%
It takes 4 to 5 half lives to reach 100 %
Area under the plasma concentration curve AUC
Aka the amount of drug that reached systemic circulation
Bioavailability
Phase 1 reactions
To make drug more polar / water soluble for excretion as urine
HOaRD water
Hydrolysis Oxidation a Reduction Deamination
Phase II reactions are Glucoronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation
Viral DNA polymerase inhibitor used in CMV retinitis when ganciclovir fails.
Foscarnet
Inhibition of neuraminidase which is necessary to release virions.
Works against influenza A and B
Zanamivir
Oseltmivir
Nucleoside analogue that inhibits the synthesis of Guanine nucleotides.
Used in RSV and Hep C (+ interferon alpha)
Ribavirin
Regimen for HIV
2 NRTI + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor
NRTI: zidovudine, didanosine, lamivudine, abacavir,
stavudine, emricitabine, tenofovir - no activation reqd
Protease inhibitors: “-navir” drugs
NNRTI: nevirapine, efavirenz, delavirdine. DEFeN need activation
Integrase inhibitor: Raltegravir
Prevent maturation of new virus
Protease inhibitor
Inhibit HIV genome integration into host cell
Integrase inhibitor - Raltegravir
Allergic to TMP SMX, what is the alternative for P jirovenci
Pentamidine or dapsone
Blocks peptidoglycan synthesis
Vs
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking
Blocks peptidoglycan synthesis - vancomycin by binding D Ala D Ala part of cell wall precursors
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking - PCN
Hepatitis B medication
Lamivudine + interferon alpha
Cephalosporin effective against Pseudomonas aeruginosa 3
1 cefoPERAzone 3 gen
2 ceftaziDIME 3 gen
3 CEFEpime 4 gen
CE FE ang PERA DIME
Anti HIV drug tha decrease mother to fetus transmission of HiV
Zidovudine
MOA clindamycin
Blocks peptide bond formation at the 50sS ribosomal subunit
Clindamycin - prevents bond formation so no new bacteria is produced : BACTERIOSTATIC
Indication: methicillin resistant Staph aureus
Inhibits 50s peptidyltransferase
Chloramphenicol
Meningitis: H influenza, N meningitidis, S pneumonia
SE
Gray baby syndrome - lack of liver UDP glucuronyl transferase
Anemia/Aplastic anemia
Medication for Alzheimer’s that inhibits cholinesterase ie indirect cholinomimetic.
Donepezil
Not a cure, slows down disease but does not alter course.
Multinucleated giant cells. After initial infection, travels in retrograde manner to DRG.
Enveloped ds DNA virus.
HSV
Tzank smear
CYP 450 Inhibitors
Quin V inhibited was SICK with RAGE
Quinidine V inhibited was Sulfonamides Isoniazid Cimetidine Ketoconazole Riot avid Amniodarone Grapefruit Erythromycin
CYP 450 Inducers
Momma Ethel Booba Phoned Refusing Smoked or Grilled Carp
Modafinil Ethanol Barbidurates Phenytoin aka phenobarbiedoll Rifampicin Smoking or St. John's wort Griseofulvin Carbamazepine
Bactericidal antibiotics
Very Finely Proficient At Murder
Vancomycin - binds D ala D ala Fluroquinolone - inhibits DNA gyrase PCN - bind transpeptidase Aminoglycoside - inhibits initiation complex , 30s Metronidazole -
Bacteriostatic antibiotics
BacteriostaTTECCS
Trimethoprim Tetracycline Erythromycin Clindamycin Chloramphenicol Sulfamethoxazole
Antifungal: disrupts membrane function
Amphotheracin B
Nystatin
Antifungal: disrupts cell wall synthesis
Caspofungin
Anidulfungin
Antifungal: disrupts ergosterol synthesis
Fluconazole
Itraconazole
Voriconazole
Antifungal: disrupts lanosterol synthesis
Terbinafine
Naftifine
SE of protease inhibitors “navir”s used in HIV tx
Lipodystrophy - fat redistribution
Hyperglycemia
GI intolerance, Nephropathy, Hematuria (indinavir)
Lopinavir, Atazanavir, Ritonavir, Indinavir, etc
Nucleoside reverse transcriptase inhibitors NRTI side effect.
Bone marrow suppression
Peripheral neuropathy
Anemia - zidovudine
Didanosine, lamivudine, abacavir, tenofovir, zidovudine formerly azt,
Effect of drug on body
PharmacoDynamics
Effect of body on the drug
Pharmacokinetics
of hours max for pralidoxime to work
6 to 8 hrs
Used like atropine for organophosphate poisoning
Used to alkalinize or acidify urine
alkalinize urine - make it Basic with Bicarbonate
acidify urine - make it Acidic with Ammonium chloride
Sublingual hypertensive meds pathway
Lingual vein -> IJV -> brachiocephalic or innominate vein -> SVC -> RA
Rectal route of meds partial first pass because
Superior rectal vain -> IMV -> portal system FIRST PASS
Middle rectal vein -> IIV -> IVC
Inferior rectal vein -> IPV -> IIV -> IVC
Best topical preparation
Ointment > foam > cream
Slowest drug route
Routes of administration
Significant first pass effect ?
Partially bypasses first pass effect ?
Completely bypasses first pass effect ?
Significant first pass effect ? Oral
Partially bypasses first pass effect ? Rectal
Completely bypasses first pass effect ? IV, IM, SC, SL, inhalation, topical, transdermal (systemic effect)
Soluble drugs are _____ & ________
Non ionized and non polar aka lipid soluble
Drugs that have zero order kinetics ie constant elimination rate over time / Linear
WHAT PET
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Note. NO Half life in zero order!!!
Dosage required to have 50% efficacy aka amount needed to produce a given effect.
Potency
Efficacy is the height of the curve, potency is concentration in x axis
Concentration required to bind 50% of receptors
Kd
High Kd, low affinity etc
Measures of potency
ED50 median effective
TD50 median toxic
LD50 median lethal
Agonist + competitive antagonist
Dec potency but same efficacy.
Lower Kmax, same Vmax
Shift to the right. You need more to obtain same effect in presence of competitive antagonist.
Agonist plus concompetitive antagonist
DECrease efficacy, with same potency.
Lower Vmax, same Kd
Idiosyncratic effect of allopurinol
Cataract
First order kinetics. Drugs metabolized 1, 2, 3 half life
1st half life 50%
2nd half life 75 %
3rd half life 87.5%
It takes 4 to 5 half lives to reach 100 %
Area under the plasma concentration curve AUC
Aka the amount of drug that reached systemic circulation
Bioavailability
Phase 1 reactions
To make drug more polar / water soluble for excretion as urine
HOaRD water
Hydrolysis Oxidation a Reduction Deamination
Phase II reactions are Glucoronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation
Viral DNA polymerase inhibitor used in CMV retinitis when ganciclovir fails.
Foscarnet
Inhibition of neuraminidase which is necessary to release virions.
Works against influenza A and B
Zanamivir
Oseltmivir
Nucleoside analogue that inhibits the synthesis of Guanine nucleotides.
Used in RSV and Hep C (+ interferon alpha)
Ribavirin
Regimen for HIV
2 NRTI + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor
NRTI: zidovudine, didanosine, lamivudine, abacavir,
stavudine, emricitabine, tenofovir - no activation reqd
Protease inhibitors: “-navir” drugs
NNRTI: nevirapine, efavirenz, delavirdine. DEFeN need activation
Integrase inhibitor: Raltegravir
Prevent maturation of new virus
Protease inhibitor
Inhibit HIV genome integration into host cell
Integrase inhibitor - Raltegravir
Allergic to TMP SMX, what is the alternative for P jirovenci
Pentamidine or dapsone
Blocks peptidoglycan synthesis
Vs
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking
Blocks peptidoglycan synthesis - vancomycin by binding D Ala D Ala part of cell wall precursors
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking - PCN
Hepatitis B medication
Lamivudine + interferon alpha
Cephalosporin effective against Pseudomonas aeruginosa 3
1 cefoPERAzone 3 gen
2 ceftaziDIME 3 gen
3 CEFEpime 4 gen
CE FE ang PERA DIME
Anti HIV drug tha decrease mother to fetus transmission of HiV
Zidovudine
MOA clindamycin
Blocks peptide bond formation at the 50sS ribosomal subunit
Clindamycin - prevents bond formation so no new bacteria is produced : BACTERIOSTATIC
Indication: methicillin resistant Staph aureus
Inhibits 50s peptidyltransferase
Chloramphenicol
Meningitis: H influenza, N meningitidis, S pneumonia
SE
Gray baby syndrome - lack of liver UDP glucuronyl transferase
Anemia/Aplastic anemia
Medication for Alzheimer’s that inhibits cholinesterase ie indirect cholinomimetic.
Donepezil
Not a cure, slows down disease but does not alter course.
Multinucleated giant cells. After initial infection, travels in retrograde manner to DRG.
Enveloped ds DNA virus.
HSV
Tzank smear
CYP 450 Inhibitors
Quin V inhibited was SICK with RAGE
Quinidine V inhibited was Sulfonamides Isoniazid Cimetidine Ketoconazole Riot avid Amniodarone Grapefruit Erythromycin
CYP 450 Inducers
Momma Ethel Booba Phoned Refusing Smoked or Grilled Carp
Modafinil Ethanol Barbidurates Phenytoin aka phenobarbiedoll Rifampicin Smoking or St. John's wort Griseofulvin Carbamazepine
Bactericidal antibiotics
Very Finely Proficient At Murder
Vancomycin - binds D ala D ala Fluroquinolone - inhibits DNA gyrase PCN - bind transpeptidase Aminoglycoside - inhibits initiation complex , 30s Metronidazole -
Bacteriostatic antibiotics
BacteriostaTTECCS
Trimethoprim Tetracycline Erythromycin Clindamycin Chloramphenicol Sulfamethoxazole
Antifungal: disrupts membrane function
Amphotheracin B
Nystatin
Antifungal: disrupts cell wall synthesis
Caspofungin
Anidulfungin
Antifungal: disrupts ergosterol synthesis
Fluconazole
Itraconazole
Voriconazole
Antifungal: disrupts lanosterol synthesis
Terbinafine
Naftifine
SE of protease inhibitors “navir”s used in HIV tx
Lipodystrophy - fat redistribution
Hyperglycemia
GI intolerance, Nephropathy, Hematuria (indinavir)
Lopinavir, Atazanavir, Ritonavir, Indinavir, etc
Nucleoside reverse transcriptase inhibitors NRTI side effect.
Bone marrow suppression
Peripheral neuropathy
Anemia - zidovudine
Didanosine, lamivudine, abacavir, tenofovir, zidovudine formerly azt,
Effect of drug on body
PharmacoDynamics
Effect of body on the drug
Pharmacokinetics
of hours max for pralidoxime to work
6 to 8 hrs
Used like atropine for organophosphate poisoning
Used to alkalinize or acidify urine
alkalinize urine - make it Basic with Bicarbonate
acidify urine - make it Acidic with Ammonium chloride
Sublingual hypertensive meds pathway
Lingual vein -> IJV -> brachiocephalic or innominate vein -> SVC -> RA
Rectal route of meds partial first pass because
Superior rectal vain -> IMV -> portal system FIRST PASS
Middle rectal vein -> IIV -> IVC
Inferior rectal vein -> IPV -> IIV -> IVC
Best topical preparation
Ointment > foam > cream
Slowest drug route
Routes of administration
Significant first pass effect ?
Partially bypasses first pass effect ?
Completely bypasses first pass effect ?
Significant first pass effect ? Oral
Partially bypasses first pass effect ? Rectal
Completely bypasses first pass effect ? IV, IM, SC, SL, inhalation, topical, transdermal (systemic effect)
Soluble drugs are _____ & ________
Non ionized and non polar aka lipid soluble
Drugs that have zero order kinetics ie constant elimination rate over time / Linear
WHAT PET
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Note. NO Half life in zero order!!!
Dosage required to have 50% efficacy aka amount needed to produce a given effect.
Potency
Efficacy is the height of the curve, potency is concentration in x axis
Concentration required to bind 50% of receptors
Kd
High Kd, low affinity etc
Measures of potency
ED50 median effective
TD50 median toxic
LD50 median lethal
Agonist + competitive antagonist
Dec potency but same efficacy.
Lower Kmax, same Vmax
Shift to the right. You need more to obtain same effect in presence of competitive antagonist.
Agonist plus concompetitive antagonist
DECrease efficacy, with same potency.
Lower Vmax, same Kd
Idiosyncratic effect of allopurinol
Cataract
First order kinetics. Drugs metabolized 1, 2, 3 half life
1st half life 50%
2nd half life 75 %
3rd half life 87.5%
It takes 4 to 5 half lives to reach 100 %
Area under the plasma concentration curve AUC
Aka the amount of drug that reached systemic circulation
Bioavailability
Phase 1 reactions
To make drug more polar / water soluble for excretion as urine
HOaRD water
Hydrolysis Oxidation a Reduction Deamination
Phase II reactions are Glucoronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation
Viral DNA polymerase inhibitor used in CMV retinitis when ganciclovir fails.
Foscarnet
Inhibition of neuraminidase which is necessary to release virions.
Works against influenza A and B
Zanamivir
Oseltmivir
Nucleoside analogue that inhibits the synthesis of Guanine nucleotides.
Used in RSV and Hep C (+ interferon alpha)
Ribavirin
Regimen for HIV
2 NRTI + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor
NRTI: zidovudine, didanosine, lamivudine, abacavir,
stavudine, emricitabine, tenofovir - no activation reqd
Protease inhibitors: “-navir” drugs
NNRTI: nevirapine, efavirenz, delavirdine. DEFeN need activation
Integrase inhibitor: Raltegravir
Prevent maturation of new virus
Protease inhibitor
Inhibit HIV genome integration into host cell
Integrase inhibitor - Raltegravir
Allergic to TMP SMX, what is the alternative for P jirovenci
Pentamidine or dapsone
Blocks peptidoglycan synthesis
Vs
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking
Blocks peptidoglycan synthesis - vancomycin by binding D Ala D Ala part of cell wall precursors
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking - PCN
Hepatitis B medication
Lamivudine + interferon alpha
Cephalosporin effective against Pseudomonas aeruginosa 3
1 cefoPERAzone 3 gen
2 ceftaziDIME 3 gen
3 CEFEpime 4 gen
CE FE ang PERA DIME
Anti HIV drug tha decrease mother to fetus transmission of HiV
Zidovudine
MOA clindamycin
Blocks peptide bond formation at the 50sS ribosomal subunit
Clindamycin - prevents bond formation so no new bacteria is produced : BACTERIOSTATIC
Indication: methicillin resistant Staph aureus
Inhibits 50s peptidyltransferase
Chloramphenicol
Meningitis: H influenza, N meningitidis, S pneumonia
SE
Gray baby syndrome - lack of liver UDP glucuronyl transferase
Anemia/Aplastic anemia
Allergic to TMP SMX, what is the alternative for P jirovenci
Pentamidine or dapsone
Blocks peptidoglycan synthesis
Vs
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking
Blocks peptidoglycan synthesis - vancomycin by binding D Ala D Ala part of cell wall precursors
Blocks cell wall synthesis by inhibiting peptidoglycan cross linking - PCN
Hepatitis B medication
Lamivudine + interferon alpha
Inhibits 50s peptidyltransferase
Chloramphenicol
Meningitis: H influenza, N meningitidis, S pneumonia
SE
Gray baby syndrome - lack of liver UDP glucuronyl transferase
Anemia/Aplastic anemia
MOA clindamycin
Blocks peptide bond formation at the 50sS ribosomal subunit
Clindamycin - prevents bond formation so no new bacteria is produced : BACTERIOSTATIC
Indication: methicillin resistant Staph aureus
Anti HIV drug tha decrease mother to fetus transmission of HiV
Zidovudine
Cephalosporin effective against Pseudomonas aeruginosa 3
1 cefoPERAzone 3 gen
2 ceftaziDIME 3 gen
3 CEFEpime 4 gen
CE FE ang PERA DIME
Medication for Alzheimer’s that inhibits cholinesterase ie indirect cholinomimetic.
Donepezil
Not a cure, slows down disease but does not alter course.
Multinucleated giant cells. After initial infection, travels in retrograde manner to DRG.
Enveloped ds DNA virus.
HSV
Tzank smear
CYP 450 Inhibitors
Quin V inhibited was SICK with RAGE
Quinidine V inhibited was Sulfonamides Isoniazid Cimetidine Ketoconazole Riot avid Amniodarone Grapefruit Erythromycin
Inhibit HIV genome integration into host cell
Integrase inhibitor - Raltegravir
Prevent maturation of new virus
Protease inhibitor
Regimen for HIV
2 NRTI + 1 NNRTI or 1 protease inhibitor or 1 integrase inhibitor
NRTI: zidovudine, didanosine, lamivudine, abacavir,
stavudine, emricitabine, tenofovir - no activation reqd
Protease inhibitors: “-navir” drugs
NNRTI: nevirapine, efavirenz, delavirdine. DEFeN need activation
Integrase inhibitor: Raltegravir
Nucleoside analogue that inhibits the synthesis of Guanine nucleotides.
Used in RSV and Hep C (+ interferon alpha)
Ribavirin
Inhibition of neuraminidase which is necessary to release virions.
Works against influenza A and B
Zanamivir
Oseltmivir
Viral DNA polymerase inhibitor used in CMV retinitis when ganciclovir fails.
Foscarnet
Phase 1 reactions
To make drug more polar / water soluble for excretion as urine
HOaRD water
Hydrolysis Oxidation a Reduction Deamination
Phase II reactions are Glucoronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation
Area under the plasma concentration curve AUC
Aka the amount of drug that reached systemic circulation
Bioavailability
First order kinetics. Drugs metabolized 1, 2, 3 half life
1st half life 50%
2nd half life 75 %
3rd half life 87.5%
It takes 4 to 5 half lives to reach 100 %
Idiosyncratic effect of allopurinol
Cataract
Agonist plus concompetitive antagonist
DECrease efficacy, with same potency.
Lower Vmax, same Kd
Agonist + competitive antagonist
Dec potency but same efficacy.
Lower Kmax, same Vmax
Shift to the right. You need more to obtain same effect in presence of competitive antagonist.
Measures of potency
ED50 median effective
TD50 median toxic
LD50 median lethal
Concentration required to bind 50% of receptors
Kd
High Kd, low affinity etc
Dosage required to have 50% efficacy aka amount needed to produce a given effect.
Potency
Efficacy is the height of the curve, potency is concentration in x axis
Drugs that have zero order kinetics ie constant elimination rate over time / Linear
WHAT PET
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Note. NO Half life in zero order!!!
Soluble drugs are _____ & ________
Non ionized and non polar aka lipid soluble
Routes of administration
Significant first pass effect ?
Partially bypasses first pass effect ?
Completely bypasses first pass effect ?
Significant first pass effect ? Oral
Partially bypasses first pass effect ? Rectal
Completely bypasses first pass effect ? IV, IM, SC, SL, inhalation, topical, transdermal (systemic effect)
Best topical preparation
Ointment > foam > cream
Slowest drug route
Rectal route of meds partial first pass because
Superior rectal vain -> IMV -> portal system FIRST PASS
Middle rectal vein -> IIV -> IVC
Inferior rectal vein -> IPV -> IIV -> IVC
Sublingual hypertensive meds pathway
Lingual vein -> IJV -> brachiocephalic or innominate vein -> SVC -> RA
Used to alkalinize or acidify urine
alkalinize urine - make it Basic with Bicarbonate
acidify urine - make it Acidic with Ammonium chloride
of hours max for pralidoxime to work
6 to 8 hrs
Used like atropine for organophosphate poisoning
CYP 450 Inducers
Momma Ethel Booba Phoned Refusing Smoked or Grilled Carp
Modafinil Ethanol Barbidurates Phenytoin aka phenobarbiedoll Rifampicin Smoking or St. John's wort Griseofulvin Carbamazepine
Effect of body on the drug
Pharmacokinetics
Effect of drug on body
PharmacoDynamics
Nucleoside reverse transcriptase inhibitors NRTI side effect.
Bone marrow suppression
Peripheral neuropathy
Anemia - zidovudine
Didanosine, lamivudine, abacavir, tenofovir, zidovudine formerly azt,
SE of protease inhibitors “navir”s used in HIV tx
Lipodystrophy - fat redistribution
Hyperglycemia
GI intolerance, Nephropathy, Hematuria (indinavir)
Lopinavir, Atazanavir, Ritonavir, Indinavir, etc
Antifungal: disrupts lanosterol synthesis
Terbinafine
Naftifine
Antifungal: disrupts ergosterol synthesis
Fluconazole
Itraconazole
Voriconazole
Bactericidal antibiotics
Very Finely Proficient At Murder
Vancomycin - binds D ala D ala Fluroquinolone - inhibits DNA gyrase PCN - bind transpeptidase Aminoglycoside - inhibits initiation complex , 30s Metronidazole -
Antifungal: disrupts cell wall synthesis
Caspofungin
Anidulfungin
Antifungal: disrupts membrane function
Amphotheracin B
Nystatin
Bacteriostatic antibiotics
BacteriostaTTECCS
Trimethoprim Tetracycline Erythromycin Clindamycin Chloramphenicol Sulfamethoxazole
DOC for PCP ?
If with sulfa allergy?
DOC for PCP ? TMP-SMX (tx and prophylaxis)
If with sulfa allergy? Pentamidine
Prophylaxis for CD<200 in HIV
Antibiotics versus Pseudomonas aeruginosa
Ce Fe Pera Dime
- CEFEpime
- CefoPERAzime
- CeftaziDIME
Extended spectrum PCN + Aminoglycoside
-Aminoglycoside + Ticarcillin/Carbenicillin/Piperacillin
Long term medication for chronic atrial fibrillation
Warfarin
INT 2-3
Prevents further clot formation?
Breaks down existing clots?
Interferes with the binding of fibrinogen to platelets?
Binds glycoprotein receptor IIb/IIIa on activated platelets?
Prevents further clot formation? Heparin and ASA
- does NOT break down existing clots!!!
- Heparin: catalyzed activation of anti thrombin III
- ASA side effect: tinnitus
Breaks down existing clots?
Thrombolytics: streptokinase/tissue plasminogen activator tPA
- converts plasminogen to PLASMIN which cleaves thrombin and fibrin clots
Interferes with the binding of fibrinogen to platelets?
Clopidogrel and ticlopidine
- via inhibiting the ADP pathway
Binds glycoprotein receptor IIb/IIIa on activated platelets?
Abciximab: prevents platelet aggregation
Blocks leukotriene receptors?
Inhibits the 5 lipoxygenase pathway preventing conversion of arachidonic acid to leukotrienes?
Blocks leukotriene receptors? Zafirlukast
Inhibits the 5 lipoxygenase pathway? Zileuton
Epinephrine vs Phentolamine
Epinephrine : nonselective agonist of Alpha and Beta receptors
Phentolamine : nonselective Alpha antagonist
if you give Epi alone, net inc in BP
- B1 HR,inc contractility
- A1 inc TPR (B mediated vasodilation negligible compared to A1 effects)
If you give Phentolamine alone, net inc BP
- B1 HR,inc contractility
- Normal Beta mediated vasodilation, no alpha action
If you give Epi then Phentolamine, net effect: Dec BP
- No Alpha actions, Increased Beta action from Epi
- arterioles: only Beta acting so massive vasodilation = Dec BP
- Inc HR and Contractility
Epi vs NorE vs Isoproterenol vs Dopa vs DoBu vs Phenylephrine vs Ritodrine vs Salmetrol/Terbutaline/Albuterol
A1 A2 B1 B2 D1
Epi +++ +++ ++++ ++++ 0
NorE ++++ ++++ ++ 0 0
Isoproterenol 0 0 ++++ ++++ 0
Dopa +++ H +++H +++M ++M +++L
DoBu + + ++++ + 0
Phenylephrine +++ ++ 0 0 0
Ritodrine 0 0 0 ++++ 0
Salmetrol/ 0 0 ++ ++++ 0
Terbutaline/
Albuterol
Un intended effect of Norepinephrine
Decrease HR
- NorE inc venous return to heart, via vasoconstriction and inc HR causing Inc SV. Since heart no longer needs to beat fast to maintain sufficient CO (SV x HR), there is REFLEX Bradycardia
Oncology drugs
Induces formation of free radicals during the G2 phase?
Cross links chloride group during active and resting phase?
Inhibits topoisomerase II during the late S and early G2 phase?
Induces formation of free radicals at G2 phase causing DNA strand breaks?
- Bleomycin: pulmonary fibrosis: testicular Ca : lymphoma
Cross links chloride group during active and resting phase?
- Cisplatin: alkylating agent: cell cycle non specific : ototoxicity
Inhibits topoisomerase II ( unwinds DNA) during the late S and early G2 phase?
- Etoposide: increases DNA degradation
SE leukopenia/neutropenia/alopecia
Antifungals
Disrupts microtubule function?
Forms pores in the cell membrane?
Inhibit DNA synthesis?
Inhibits conversion of lanosterol to ergosterol?
Inhibits conversion of squalene to lanosterol?
Disrupts microtubule function? Griseofulvin
Forms pores in the cell membrane? AmPOREthericin
- binds to ergosterol in cell membrane and creates pores
Inhibit DNA synthesis? Flucystosine
- Pyrimidine anti metabolite like 5FU
- competes with uracil
Inhibits conversion of lanosterol to ergosterol? Azoles
- inhibit 14 alpha due methylation of lanosterol
- ketoconazole, fluconazole
Inhibits conversion of squalene to lanosterol? Terbinafine
- inhibits squalene epoxidase
Indication for Cox 2 inhibitors
Patients with known inflammation who are at high risk for GI ulceration and are at LOW RISK for CARDIOvascular ds
COX 1 gastric cytoprotection
COX 2 inflammatory state
- in general , non specific COX inhibitors block conversion of AA to endoperoxides precursor of Prostaglandin, Prostacyclin, Thromboxane.
- Prostacyclin is a powerful vasodilator and inhibitor of platelet aggregation. Thromboxane is a powerful vasoconstrictor and promoter of platelet aggreation.
- COX 2 inhibitor increases CVS risk because it decreases Prostacyclin without corresponding decrease in Thromboxane
Pulmonary fibrosis causing drugs
Bleomycin
Busulfan
Methotrexate
Nitrofurantoin
P450 inducers
Momma Bar Steals Phen phen and Refuses Greasy Carbs Chronically
Modanifil Barbidurates St Johns wort Phenytoin Griseofulvin Carbamazepine Chronic alcohol use
Drugs that precipitate hemolysis in G6PD
Sulfonamides Isoniazid Aspirin Ibuprofen Primaquine Nitrofurantoin
Monoamine oxidase inhibitors
“MAO Takes Pride In Shanghai”
MAO inhibitors inc NE, Serotonin, Dopamine Tranylcypromine Phenelzine Isocarboxazid Selegiline
Toxicity: serotonin syndrome on exposure to certain food
Toxicity of TCA: excess acetylcholine symptoms
MOA of Doxorubicin and Daunorubicin
DNA intercalators that act by binding to DNA and disrupting nucleic acid synthesis.
Via “ no covalent intercalation with DNA”
SE dilated cardiomyopathy
MOA of 6 Mercaptopurine
Acts as a false metabolite and blocks purine synthesis
SE myelosupression, gastrointestinal effects, liver toxicity
SE
Cinchonism
Cutaneous flushing
Hemolytic anemia
Photosensitivity
Thrombocytopenia
Cinchonism (blurred vision,tinnitus,HA,disorientation) : Quinidine
Cutaneous flushing : vancomycin, adenosine, niacin, Ca blockers
Hemolytic anemia: ribavirin
Photosensitivity: sulfonamide s, Amiodarone, tetracycline
Thrombocytopenia/neutropenia/leukopenia/nephrotoxicity: Ganciclovir
Causes of folic acid deficiency
1 diet
2 phenytoin
Site of action
Bleomycin Etoposide 5 Fluorouracil Methotrexate Paclitaxel Vincristine
Bleomycin : G2 phase : causes DNA strand breaks
Etoposide : late S and G2 phase : inhibits topoisomerase II
5 Fluorouracil : S phase : inhibit thymidylate synthase
Methotrexate : S phase : inhibit dihydrofolate reductase
Paclitaxel : Metaphase
Vincristine : Metaphase
Chemo drugs
Causes covalent interstrand cross links in DNS?
Generates free radicals that intercalated DNA?
Causes covalent interstrand cross links in DNS?
- cyclophosphamide
Generates free radicals that intercalated DNA?
- Doxorubicin/Adriamycin
Used in post renal transplant to inhibit Interleukin 2 secretion
Tacrolimus
Chemo drugs
Cross links DNS?
Intercalates DNA?
Cross links DNS? Cisplatin
Intercalates DNA? Doxorubicin, et al
SE. Ganciclovir vs Ribavirin
Ganciclovir : leukopenia, neutropenia, thrombocytopenia
Ribavirin : hemolytic anemia (Coombs negative)
DOC for PCP ?
If with sulfa allergy?
DOC for PCP ? TMP-SMX (tx and prophylaxis)
If with sulfa allergy? Pentamidine
Prophylaxis for CD<200 in HIV
Antibiotics versus Pseudomonas aeruginosa
Ce Fe Pera Dime
- CEFEpime
- CefoPERAzime
- CeftaziDIME
Extended spectrum PCN + Aminoglycoside
-Aminoglycoside + Ticarcillin/Carbenicillin/Piperacillin
Long term medication for chronic atrial fibrillation
Warfarin
INT 2-3
Prevents further clot formation?
Breaks down existing clots?
Interferes with the binding of fibrinogen to platelets?
Binds glycoprotein receptor IIb/IIIa on activated platelets?
Prevents further clot formation? Heparin and ASA
- does NOT break down existing clots!!!
- Heparin: catalyzed activation of anti thrombin III
- ASA side effect: tinnitus
Breaks down existing clots?
Thrombolytics: streptokinase/tissue plasminogen activator tPA
- converts plasminogen to PLASMIN which cleaves thrombin and fibrin clots
Interferes with the binding of fibrinogen to platelets?
Clopidogrel and ticlopidine
- via inhibiting the ADP pathway
Binds glycoprotein receptor IIb/IIIa on activated platelets?
Abciximab: prevents platelet aggregation
Blocks leukotriene receptors?
Inhibits the 5 lipoxygenase pathway preventing conversion of arachidonic acid to leukotrienes?
Blocks leukotriene receptors? Zafirlukast
Inhibits the 5 lipoxygenase pathway? Zileuton
Epinephrine vs Phentolamine
Epinephrine : nonselective agonist of Alpha and Beta receptors
Phentolamine : nonselective Alpha antagonist
if you give Epi alone, net inc in BP
- B1 HR,inc contractility
- A1 inc TPR (B mediated vasodilation negligible compared to A1 effects)
If you give Phentolamine alone, net inc BP
- B1 HR,inc contractility
- Normal Beta mediated vasodilation, no alpha action
If you give Epi then Phentolamine, net effect: Dec BP
- No Alpha actions, Increased Beta action from Epi
- arterioles: only Beta acting so massive vasodilation = Dec BP
- Inc HR and Contractility
Epi vs NorE vs Isoproterenol vs Dopa vs DoBu vs Phenylephrine vs Ritodrine vs Salmetrol/Terbutaline/Albuterol
A1 A2 B1 B2 D1
Epi +++ +++ ++++ ++++ 0
NorE ++++ ++++ ++ 0 0
Isoproterenol 0 0 ++++ ++++ 0
Dopa +++ H +++H +++M ++M +++L
DoBu + + ++++ + 0
Phenylephrine +++ ++ 0 0 0
Ritodrine 0 0 0 ++++ 0
Salmetrol/ 0 0 ++ ++++ 0
Terbutaline/
Albuterol
Un intended effect of Norepinephrine
Decrease HR
- NorE inc venous return to heart, via vasoconstriction and inc HR causing Inc SV. Since heart no longer needs to beat fast to maintain sufficient CO (SV x HR), there is REFLEX Bradycardia
Oncology drugs
Induces formation of free radicals during the G2 phase?
Cross links chloride group during active and resting phase?
Inhibits topoisomerase II during the late S and early G2 phase?
Induces formation of free radicals at G2 phase causing DNA strand breaks?
- Bleomycin: pulmonary fibrosis: testicular Ca : lymphoma
Cross links chloride group during active and resting phase?
- Cisplatin: alkylating agent: cell cycle non specific : ototoxicity
Inhibits topoisomerase II ( unwinds DNA) during the late S and early G2 phase?
- Etoposide: increases DNA degradation
SE leukopenia/neutropenia/alopecia
Antifungals
Disrupts microtubule function?
Forms pores in the cell membrane?
Inhibit DNA synthesis?
Inhibits conversion of lanosterol to ergosterol?
Inhibits conversion of squalene to lanosterol?
Disrupts microtubule function? Griseofulvin
Forms pores in the cell membrane? AmPOREthericin
- binds to ergosterol in cell membrane and creates pores
Inhibit DNA synthesis? Flucystosine
- Pyrimidine anti metabolite like 5FU
- competes with uracil
Inhibits conversion of lanosterol to ergosterol? Azoles
- inhibit 14 alpha due methylation of lanosterol
- ketoconazole, fluconazole
Inhibits conversion of squalene to lanosterol? Terbinafine
- inhibits squalene epoxidase
Indication for Cox 2 inhibitors
Patients with known inflammation who are at high risk for GI ulceration and are at LOW RISK for CARDIOvascular ds
COX 1 gastric cytoprotection
COX 2 inflammatory state
- in general , non specific COX inhibitors block conversion of AA to endoperoxides precursor of Prostaglandin, Prostacyclin, Thromboxane.
- Prostacyclin is a powerful vasodilator and inhibitor of platelet aggregation. Thromboxane is a powerful vasoconstrictor and promoter of platelet aggreation.
- COX 2 inhibitor increases CVS risk because it decreases Prostacyclin without corresponding decrease in Thromboxane
Pulmonary fibrosis causing drugs
Bleomycin
Busulfan
Methotrexate
Nitrofurantoin
P450 inducers
Momma Bar Steals Phen phen and Refuses Greasy Carbs Chronically
Modanifil Barbidurates St Johns wort Phenytoin Griseofulvin Carbamazepine Chronic alcohol use
Drugs that precipitate hemolysis in G6PD
Sulfonamides Isoniazid Aspirin Ibuprofen Primaquine Nitrofurantoin
Monoamine oxidase inhibitors
“MAO Takes Pride In Shanghai”
MAO inhibitors inc NE, Serotonin, Dopamine Tranylcypromine Phenelzine Isocarboxazid Selegiline
Toxicity: serotonin syndrome on exposure to certain food
Toxicity of TCA: excess acetylcholine symptoms
MOA of Doxorubicin and Daunorubicin
DNA intercalators that act by binding to DNA and disrupting nucleic acid synthesis.
Via “ no covalent intercalation with DNA”
SE dilated cardiomyopathy
MOA of 6 Mercaptopurine
Acts as a false metabolite and blocks purine synthesis
SE myelosupression, gastrointestinal effects, liver toxicity
SE
Cinchonism
Cutaneous flushing
Hemolytic anemia
Photosensitivity
Thrombocytopenia
Cinchonism (blurred vision,tinnitus,HA,disorientation) : Quinidine
Cutaneous flushing : vancomycin, adenosine, niacin, Ca blockers
Hemolytic anemia: ribavirin
Photosensitivity: sulfonamide s, Amiodarone, tetracycline
Thrombocytopenia/neutropenia/leukopenia/nephrotoxicity: Ganciclovir
Causes of folic acid deficiency
1 diet
2 phenytoin
Site of action
Bleomycin Etoposide 5 Fluorouracil Methotrexate Paclitaxel Vincristine
Bleomycin : G2 phase : causes DNA strand breaks
Etoposide : late S and G2 phase : inhibits topoisomerase II
5 Fluorouracil : S phase : inhibit thymidylate synthase
Methotrexate : S phase : inhibit dihydrofolate reductase
Paclitaxel : Metaphase
Vincristine : Metaphase
Chemo drugs
Causes covalent interstrand cross links in DNS?
Generates free radicals that intercalated DNA?
Causes covalent interstrand cross links in DNS?
- cyclophosphamide
Generates free radicals that intercalated DNA?
- Doxorubicin/Adriamycin
Used in post renal transplant to inhibit Interleukin 2 secretion
Tacrolimus
Chemo drugs
Cross links DNS?
Intercalates DNA?
Cross links DNS? Cisplatin
Intercalates DNA? Doxorubicin, et al
SE. Ganciclovir vs Ribavirin
Ganciclovir : leukopenia, neutropenia, thrombocytopenia
Ribavirin : hemolytic anemia (Coombs negative)