Drugs Flashcards
Terbinafine
Antifungal
Inhibits squalene epoxidase (necessary for formation of lanosterol which then becomes ergosterol)
Azoles
Antifungal
Inhibits 14a-demethylase (converts lanosterol to ergosterol)
Flucytosine
Antifungal
Inhibits nucleic acid synthesis in fungal cells
Causes bone marrow suppression
Amphotericin B
Antifungal
Forms membrane pores in fungal cells (“ters” holes in the membrane)
Causes hypotension, renal toxicity, IV phlebitis, fever/chills
Echinocandins
Antifungal
Inhibits B glucan synthesis and disrupts the cell wall
Griseofulvin
Antifungal (used for nail fungal infections)
Interferes with microtubule function and disrupts mitosis
Acyclovir
Antiviral (used for herpes virus infections)
Viral dependent nucleoside
Converted to monophosphate form by viral kinase and then to triphosphate form by host cell kinase –> inhibits DNA polymerase and causes chain termination
**Resistance occurs when there is an absence of viral thymidine kinase
Ganciclovir
Antiviral (used for herpes virus infections)
specifically used for CMV infection
Viral dependent nucleoside
Converted to monophosphate form by viral kinase and then to triphosphate form by host cell kinase –> inhibits DNA polymerase and causes chain termination
**Resistance occurs when there is an absence of viral thymidine kinase
Valacyclovir
Antiviral (used for herpes virus infections)
Used to prevent reactivation of HSV
Viral dependent nucleoside
Converted to monophosphate form by viral kinase and then to triphosphate form by host cell kinase –> inhibits DNA polymerase and causes chain termination
**Resistance occurs when there is an absence of viral thymidine kinase
Cidovir
Antiviral (herpes virus)
Only needs to be activated by host cell kinases to be activated–> inhibits DNA polymerase and causes chain termination
Tenofovir
Antiviral (herpes virus)
Only needs to be activated by host cell kinases to be activated–> inhibits DNA polymerase and causes chain termination
Zidovudine
Antiviral (herpes virus)
Cell dependent nucleoside
Only needs to be activated by host cell kinases to be activated–> inhibits DNA polymerase and causes chain termination
Lamivudine
Antiviral (herpes virus)
Cell dependent nucleoside
Only needs to be activated by host cell kinases to be activated–> inhibits DNA polymerase and causes chain termination
Celecoxib
Irreversible COX-2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
Has decreased side effects than other NSAIDs but has increased cardio risks
Aspirin
Irreversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Do not give to kids with the flu –> can cause Reyes syndrome (encephalitis, fatty liver, liver failure) because it uncouples oxidative phosphorylation and disrupts the proton gradient along the e- transport chain
Ibuprofen
Reversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Diclofenac
Reversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Indomethacin
Reversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Ketorolac
Reversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Naproxen
Reversible COX 1/2 inhibitor
Prevents AA –> prostaglandins (normally sensitize pain fibers)
GI irritation, GERD, GI ulcers
Corticosteroids (Prednisone, Dexamethasone, Betamethasone, etc)
Inhibit phospholipase A2 (via increase of lipocortin) to prevent formation of arachidonic acid
Causes immunosuppression, Cushing’s syndrome, thinning of skin (if used topically)
What is the first line drug for absence seizures?
Ethosuximide
“It SUX to have Silent Seizures”
Blocks Ca2+ channels
Side effects: EFGHIJ
Ethosuximide causes Fatigue, GI distress, Headache, Itching, and stevens-Johnson syndrome
What is the first line drug for control of tonic clonic seizures?
Phenytoin (inc Na channel inactivation) Carbamazepine (inc Na channel inactivation) Valproic Acid (inc Na channel inactivation, inc GABA by inhibiting GABA transaminase)
What drug do you give for acute status epilepticus?
Benzodiazepines (Diazepam, Lorazepam)
Inc GABA action by inc frequency of Cl channel opening
Side effects of Valproic Acid
Rare but fatal hepatotoxicity
Neural tube defects (teratogen)
What is a severe but uncommon side effect of Carbamazepine
Blood dyscrasias (agranulocytosis, aplastic anemia)
What do you use to treat eclampsia?
MgSO4 is first line. Can also use benzodiazepines
Local anesthetics (amides)
Blocks Na channels
Loss of 1) pain 2) temperature 3) touch 4) pressure
Succinylcholine
Neuromuscular blocker : used for muscle paralysis in surgery or mechanical ventilation
Strong ACh agonist: causes unregulated release of Ca2+ from the sarcoplasmic reticulum
Can cause malignant hyperthermia, hypercalcemia, or hyperkalemia
Rocuronium, pancuronium
Neuromuscular blocker : used for muscle paralysis in surgery or mechanical ventilation
Competes with ACh for receptors
Reverse with Neostigmine
Dantrolene
Given to correct malignant hyperthermia
Prevents release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle
What drugs can cause gynecomastia?
“Some Drugs Create Awesome Knockers”
Spironolactone: diuretic, blocks Na/K channel in collecting duct
Digoxin:
Cimetidine: H2 antagonist (Peptic ulcer disease)
Alcohol
Ketoconazole: antifungal that prevents ergosterol synthesis
Treatment of Parkinsons
BLASTA Bromocriptine Levodopa (with carbidopa) Amantadine Selegiline Tolcapone Antimuscarinics
Bromocriptine
Tx of Parkinson’s
Dopamine agonist
Amantadine
Tx of Parkinson’s
Inc dopamine availability
(inc dopamine release and dec dopamine reuptake)
Levodopa/Carbidopa
Tx of Parkinson’s
Levodopa is a precursor to dopamine and can cross the BBB. Administered with Carbidopa to prevent levodopa from turning into dopamine before it crosses the BBB (bc dopamine cannot cross the BBB)
Long term use can lead to dyskinesias and off/on phenomenon
Selegiline
Tx of Parkinson’s and atypical depression
Prevents breakdown of dopamine by inhibiting MAO
Tolcapone
Tx of Parkinson’s
Prevents breakdown of dopamine by inhibiting COMT
Benztropine
Tx of Parkinson’s
“Park your mercedes benz”
Antimuscarinic: improves tremor and rigidity but has little effect on bradykinesia
Tetrabenazine
Tx of Huntingtons
Blocks the reuptake of dopamine into vesicles via VMAT and results in degradation of dopamine
Can lead to depression due to dec. dopamine
Haloperidol
Tx of Huntington’s
D2 receptor antagonist (prevents dopamine from turning off the indirect pathway –> leads to dec movement)
Treatment of Myasthenia Gravis
Neostigmine/physostigmine: cholinesterase inhibitor
Myasthenia gravis has autoantibodies to ACh receptors - by keeping ACh in the synaptic cleft for a longer period of time, it is more likely to outcompete the autoantibodies
Which antidepressant does not have sexual side effects?
Buproprion
“Able to have proper sex”
What drug can cause priapism in men? What is it normally used for?
Trazodone (think trazobone)
Used to tx insomnia- blocks serotonin and a1 adrenergic receptors
Venlafaxine, duloxetine
SNRIs (Serotonin-NE reuptake inhibitors)
Used to tx depression, anxiety, panic disorder, and PTSD
Can cause HTN
Duloxetine: dual (Serotonin and NE)
SSRIs
Fluoxetine
Paroxetine
Sertraline
Citalopram
Side effect of Bupropion in anorexic/bulemic patients
Seizures
What drugs can you use to treat bipolar disorder?
Valproate (valproic acid)
Lithium
Atypical psychotics
Tx of Narcolepsy
Modafinil (sounds like daffodil- allows them to dream of daffodils)
Amphetamines
Tx of PTSD
Therapy
SSRI
Treatment of delirium tremens
Benzodiazepines are first line
Diazepam, Chlordiazepoxide
What can cause lithium toxicity in a bipolar patient
Use of thiazide diuretic
Clozapine side effects
Important to monitor neutrophil levels because it can cause agranulocytsis
Acetaminophen
Cox1/Cox2 inhibitor
Can cause hepatotoxicity
During metabolism, forms a reactive intermediate called NAPQ1 that can cause necrosis. GSH normally converts this to a nontoxic form, however when there is a lot of NAPQ1 formed (ex. alcohol use) then GSH is overwhelmed
Give N-acetylcysteine to limit liver injury
Triptans
Sumatriptan
USed to treat acute migraines
Serotonin agonist that inhibit trigeminal nerve activation, prevent vasoactive peptide release, and induce vasoconstriction
Naltrexone vs Disulfiram for treatment of alcoholism
Naltrexone: blocks the mu opioid receptor, blocks the rewarding and reinforcing effects of alcohol which can reduce cravings
Nal = null cravings
Disulfiram: inhibits aldehyde dehydrogenase and has an aversive mechanism of action (N/V. sweating, HA, dyspnea) but does not reduce cravings
Digoxin
Used for chronic HF (does not improve survivability)
Blocks the Na/K ATPase, which indirectly blocks the Na/Ca Exchanger – leading to inc intracellular calcium and inc contractility
Antidote: Anti-digoxin Fab fragments
