Pharmacology Flashcards
Gentamycin Neomycin Amikacin Tobramycin Streptomycinn Paromycin
Aminoglycosides
Bactericidal, inhibit 30S, only works in aerobes
What effect does Omeprazole have on various drugs?
Omeprazole is a PPI which lowers the acidity of the stomach (increases pH)
This can affect the absorption of some drugs.
- Diphenhydramine
- Dimenhydrinate
- Chlorpheniramine
First generation H1 blockers (antihistamines)
anti-allergy, induce drowsiness, anti-motion sickness
- Loratadine
- Fexofenadine
- Desloratadine
- Cetirizine
Second generation H1 blockers (antihistamines)
do not cross BBB
anti-allergy only
Cyclophosphamide mechansim of action
cross-links DNA at guanine N-7 -> inhibiting DNA replication
- Sertraline
- Paroxetine
- Fluoxetine
- Citalopram
SSRI - blocks re-uptake of serotonin only
- Venlafaxine
- Duloxetine
SNRI - blocks re-uptake of serotonin and NE
Urinary urgency means =
What do you give to treat?
Urinary urgency means the bladder is over-contracting.
Give them a muscarinic receptor antagonist to relax the detrusor contraction.
ex)atropine, oxybutamine, tolterodine, solifenacin
Excess urination - elevated Ach or decreased Ach
elevated Ach
Parasympathetics make you Pee
Cilostazol =
phosphodiesteraes inhibitor - inhibits platelet aggregation + direct vasodilation
Reye syndrome of the liver on light microscopy =
microvesicular steatosis + reduced number of mitochondria + decreased amount of glycogen
acetaminophen toxicity on LM
centrilobular hepatic necrosis
Treatment for TCA overdose =
Sodium bicarbonate
Treats the cardiac toxicity by increasing pH and increasing intracellular Na therefore alleviating the VG Na blockade
(fixes the widening of the QRS)
D-penacillamine is a treatment for?
Copper overload
used for chelation
Deferoxamine is a treatment for?
Iron overload
used for chelation
EDTA and Dimercaprol are treatments for?
Lead overload
3 drugs for Absence seizures =
- Ethosuximide = inhibits thalamic T type Ca channels
- Valproate = increased Na channel inactivation + inhibits GABA transaminase
- Lamotrigine = inhibits VG Na channels
Status Epilepticus treatments (first, second)
First: IV lorazepam = increased frequency of GABA-A channel opening - increases inward Cl current
Second: Phenytoin = increased Na channel inactivation - decreased Na current
How do opioids hyperpolarize neurons?
Increased K out, Decreased Ca in
Is glutamate excitatory or inhibitory?
excitatory!
Succimer is used for?
Lead chelation for children with lead toxicity
Clopidogrel, Parasugrel, Ticagrelor, Ticlopidine
ADP receptor inhibitors (P2-Y12 R)
Irreversible inhibition of platelet degranulation
Abciximab
Eptifibatide
Tirofiban
GPIIb/IIIa inhibitors -> inhibition of platelet aggregation
ACE inhibitor - hyperkalemia or hypokalemia?
Hyperkalemia due to inhibition of aldosterone - increased Na out, increased K in
K sparing diuretics = (4)
Spironolactone - mineralocorticoid antagonist
Eplerenone - mineralocorticoid receptor antagonist
Triamterene - inhibits ENaC
Amiloride - inhibits ENaC
Losartan
Candesartan
Valsartan
Angiotensin II Receptor Blockers (ARBs)
Diltiazem, Verapamil
Nondihydropyridine calcium channel blockers (L-type)
toxicity of: Cisplatin/Carboplatin
- acoustic nerve damage
- nephrotoxicity
mechanism of drug: cross links DNA
toxicity of: Vincristine
-peripheral neuropathy
mechanism of drug: vinca alkaloid, binds beta-tubulin -> inhibits polymerization into microtubules -> inhibits formation of mitotic spindle
toxicity of: Bleomycin, Busulfan
-pulmonary fibrosis
mechanism of Bleomycin: induces free radical formation -> DNA breaks
mechanism of Busulfan: cross links DNA
toxicity of: Doxorubicin
_ is used to prevent toxicity
-cardiotoxcity (dilated cardiomyopathy)
mechanism of drug: generates free radicals + intercalates DNA -> breaks in the DNA -> inhibits replication
Dexrazoxane (iron chelating agent) is used to prevent cardiotoxicity
toxicity of: Trastuzumab
-cardiotoxicity
mechanism of drug: monoclonal antibody against HER-2 (c-erbB2)
toxicity of: Cyclophosphamide
toxicity is reversible via administration of _ or _
-hemorrhagic cystitis (hematuria + suprapubic pain)
mechanism of drug: cross links DNA at N7 guanine
Partially reversible via mensa and N-acetylcystine
toxicity of: 5-FU, 6-MP, Methotrexate
-myelosuppression
5FU = pyrimidine analog -> (-)thymidylate synthase 6MP = purine analog Methotrexate = folic acid analog -> (-)dihydrofolate reductase
What do you give to someone who has urinary retention?
Urinary retention means their bladder is not contracting.
Give them a muscarinic agonist to help the detrusor contract.
Function of: mensa
Partially reverses toxicity of cyclophosphamide
Function of: Dexrazoxane
Iron chelating agent. Also to prevent cardiotoxicity from Doxorubicin.
Glusine
Aspart
Lispro
used for?
Rapid acting insulin
used for postprandial control
Neutral Protamine Hagedorn (NPH)
Intermediate acting insulin
Detemir
Glargine
used for?
Long acting insulin
Used for basal control
Chlorpropamide
Tolbutamide
First generation sulfonylureas = close the K+ channel on pancreatic beta cells -> -> release endogenous insulin (+ C peptide)
Disulfiram-like reaction occurs with what class of drugs? (5)
- First generation sulfonylureas (Chlorpropamide, Tolbuamide)
- Metronidazole
- Certain Cephalosporins
- Griseofulvin
- Procarbazine
Do not drink alcohol while taking these drugs.
Disulfiram inhibits acetaldehyde dehydrogenase in the ethanol metatbolism pathway. Therefore, acetaldehyde accumulates resulting in the “hangover” symptoms.
Disulfiram is given to alcoholics to condition them to stop drinking alcohol.
Glimepiride
Glyburide
Glipizide
Second generation syulfonylureas = close the K+ channel on pancreatic beta cells -> -> release endogenous insulin (+ C peptide)
Repaglinide
Nateglinide
Meglitinides = close the K+ channel on pancreatic beta cells -> -> release endogenous insulin (+ C peptide)
Works just like sulfonylureas except these can be given to people with sulfa allergies
Pioglitazone
Rosiglitazone
Binds to PPAR-gamma (a nuclear transcription regulator)
Exenatide
Liraglutide
GLP-1 analogs = increase endogenous insulin release, decrease glucagon release
Linagliptin
Saxagliptin
Sitagliptin
Dipeptidyl Peptidase-4 inhibitors (DPP4) = increase endogenous insulin release, decrease glucagon release
Pramlintide
used for?
Amylin analog = decreases gastric emptying, decreases glucagon release
controls postprandial glucose spike
Canagliflozin
SGLT-2 inhibitor - works at the PCT
Acarbose
Miglitol
inhibitors of what enzyme?
used for?
alpha-glucosidase inhibitors - work at the intestinal brush border
controls postprandial glucose spike
Pegvisomant
Growth hormone receptor antagonist
Anastrozole
Letrozole
Exemestane
Inhibits aromatase enzyme -> decreases the peripheral conversion of androgens to estrogens
Used in the treatment of ER+ breast cancers.
Misoprostol (3 main uses)
PGE1 agonist
- increased production and secretion of gastric mucous
- maintains PDA
- off-label use of labor induction (ripens cervix) or pregnancy termination
Fomepizole
Inhibits alcohol dehydrogenase
antidote for methanol or ethylene glycol poisoning
Rotenone
-inhibits complex I in the electron transport chain
decreases proton gradient and thus blocks ATP synthesis indirectly
rotenONE
Antimycin A
-inhibits complex 3 in the electron transport chain
decreases proton gradient and thus blocks ATP synthesis indirectly
“an-3-amycin”
Cyanide (CN) and CO
-inhibit complex IV (cytochrome oxidase) in the electron transport chain
decreases proton gradient and thus blocks ATP synthesis indirectly
Oligomycin
Directly inhibits the mitochondrial ATP synthase -> increases proton gradient but no ATP is produced
2,4-Dinitrophenol
Increases permeability of the mitochondrial membrane therefore causing a decreased proton gradient but an increased O2 consumption as the electrons continue to travel down the chain to try to build up the proton gradient. No ATP synthesis due to the decreased proton gradient.
Calcitriol
active Vitamin D
given to patients who are hypocalcemic
Alendronate, Risendronate
Bisphosphonates - structurally similar to pyrophosphate
-inhibits osteoclasts -> decreases calcium release from bone
Cinacalcet
Calcimimetic - stimulates Calcium sensing receptor which decreases PTH release
ADHD treatment (2)
Stimulants (Methylphenidate, Dextroamphetamine, Methamphetamine)
Clonidine (alpha-2 agonist)
Alcohol withdrawal treatment (1)
Long acting benzodiazepines
Bipolar disorder treatment (3)
Lithium
Valproate
Atypical anti-psychotics
Bulimia Nervosa treatment (1)
SSRI (Fluoxetine)
Depression treatment (1)
SSRI
Generalized anxiety disorder (2)
SSRI
SNRI
Obsessive Compulsive Disorder (2)
SSRI
Clomipramine (TCA)
Panic Disorder (3)
SSRI
Venlafaxine (SNRI)
Benzodiazepine
PTSD (2)
SSRI
Venlafaxine (SNRI)
Social phobias (4)
SSRI
Venlafaxine (SNRI)
To improve preformance: Beta-blockers, benzodiazepine
Tourette syndrome (3)
First generation anti-psychotics (Fluphenazine, Pimozide)
Tetrabenazine (inhibits VMAT -> decreased availability of dopamine)
Clonidine (alpha-2 agonist)
Haloperidol Triflupoerazine Fluphenazine Chlorpromazine Thioridazine
high potency vs low potency
First generation anti-psychotics (typicals)
High potency = Triflupoerazine, Fluphenazine, Haloperidol
“Try to Fly High”
Low potency = Chorpromazine, Thioridazine
“Cheating Thieves are Low”
Olanzapine Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone
Second generation anti-psychotics (atypicals)
Amitriptyline Nortriptyline Imipramine Desipramine Clomipramine Doxepin Amoxapine
Tricyclic antidepressants - block re-uptake of NE and Serotonin, blocks H1 receptors, block alpha-1 receptors
- Tranylcypromine
- Phenelzine
- Isocarboxazid
- Selegiline
Monoamine oxidase inhibitors - increases levels of amine neurotransmitters in the synaptic cleft (NE, Serotonin, Dopamine)
Selegiline - is MOA-B selective
MAO-A also breaks down tyramine in the GI tract
Cyproheptadine
5HT-2 receptor antagonist
-treats serotonin syndrome
treatment for major depressive disorder that does NOT have sexual side effects
Buproprion - NE and dopamine reuptake inhibitor
Buspirone
- mechanism
- used to treat what
- Stimulates 5HT-1A receptors (non-benzodiazapine anoxytic)
- Used to treat Generalized Anxiety Disorder
Takes up to 2 weeks to take effect (slow onset)
No risk of tolerance, dependence or withdrawal
Benzodiazepines that do not need the liver to be metabolized (3)
- Lorazepam
- Oxazepam
- Temazepam
“LOT”
These drugs undergo glucoronidation directly and therefore can be given to patients with impaired liver function
Long acting benzodiazepines (3)
- Chlordiazepoxide
- Diazepam
- Flurazepam
Requires the liver to be metabolized
Short acting benzodiazepines (1)
-Triazolam
Requires the liver to be metabolized
Statins mechanism of action
- inhibits HMG-CoA Reductase enzyme so less cholesterol is synthesized
- increases LDL-receptors to pull more LDL molecules out of the serum (to try to get more cholesterol that way)
best at lowering LDL levels out of all the lipid lowering agents
MOST effective at preventing future cardiovascular events
Cholestyramine
Colestipol
Colesevelam
Bile acid resigns
-prevents intestinal absorption of bile acids
(so now the cells have to make more bile acids via cholesterol. the cholesterol-stores get used up quickly)
-increases LDL-receptors to pull more LDL molecules out of the serum (to try to get more cholesterol that way)
Ezetimibe
-prevents intestinal absorption of cholesterol
(so now the cells have to make more cholesterol. the cholesterol-stores get used up quickly)
-increases LDL-receptors to pull more LDL molecules out of the serum (to try to get more cholesterol that way)
Gemfibrozil
Clofibrate
Bezafibrate
Fenofibrate
Fibrates
- activates PPAR-alpha -> upregulates LPL at extra-hepatic sites -> increased metabolism of VLDL and chylomicrons -> decreasing serum triglyceride levels
- decrease VLDL released from the liver -> decreases circulating serum triglyceride levels
- directly upregulates synthesis of HDL
Niacin (Vitamin B3)
- decrease VLDL released from the liver -> decreases circulating serum triglyceride levels
- raises HDL levels
MOST effective at raising HDL levels
Volatile anesthetics increase or decrease cerebral blood flow?
Increase cerebral blood flow
but that is a bad thing because it increases intracerebral pressures
- Imipenem
- Meropenem
- Ertapenem
- Doripenem
Carbapenem
- broad spectrum beta-lactamase resistant
- binds to PBPs
- always administered with cilsastin
Cilastin
inhibitor of renal dihydropeptdiase I
-administered with Carbapenems to decrease their inactivation
Aztreonam
Monobactams
- beta-lactamase resistant
- binds to PBP-3
- Cefazolin
- Cephalexin
First-generation Cephalosporins
-beta-lactam drug - binds to PBPs
- Cefoxitin
- Cefaclor
- Cefotetan
- Cefuroxime
Second-generation Cephalosporins
-beta-lactam drug - binds to PBPs
- Cefotaxime
- Ceftazidime
- Ceftriaxone
Third-generation Cephalosporins
- beta-lactam drug- binds to PBPs
- resistant to beta-lactamases
-Cefepime
Fourth-generation Cephalosporins
- beta-lactam drug- binds to PBPs
- resistant to beta-lactamases
- broad-spectrum
-Ceftaroline
Fifth-generation Cephalosporins
- beta-lactam drug- binds to PBPs
- broad-spectrum
Amoxicillin
- beta-lactam drug - binds to PBPs
- beta-lactamase sensitive - can be combined with beta-lactamase inhibitors (Clavulanic Acid) to prevent this
- Dicloxacillin
- Nafcillin
- Oxacillin
- beta-lactam drug - binds to PBPs
- beta-lactamase resistant due to their bulky R groups
- Piperacillin
- Ticarcillin
- beta-lactam drug - binds to PBPs
- beta-lactamase sensitive - can be combined with beta-lactamase inhibitors to prevent this
- good to use against Pseudomonas and anaerobic bugs (Bacterioides)
Clavulanic Acid
Sulbactam
Tazobactam
Beta-lactamase inhibitors
- Levofloxacin
- Moxifloxacin
Respiratory fluoroquinolones
-treat community-acquired pneumonia and walking pneumonia
Atazanavir Darunavir Fosamprenavir Indinavir Lopinavir Ritonavir Saquinavir
Protease inhibitors - prevent maturation of new viruses
-end in “navir”
Abacavir Didanosine Emtricitabine Lamivudine Stavudine Tenoforvir Zidovudine
NTRI - competitively inhibits nucleotide binding to reverse transcriptase and terminates chain elongation because these agents (nucleosides) lack a 3’OH group
-requires phosphorylation to be active
Tenofovir - nucleotide, therefore it does not need to be phosphorylated to be active
Delavirdine
Efavirenz
Nevirapine
NNRTI - allosteric inhibition of reverse trascriptase therefore terminating chain elongation
-do not require phosporylation to be active
Raltegravir
Integrase inhibitor - inhibits HIV integrating into the host cell chromosome
Simepravir
HCV protease inhibitor (NS3/4A protease inhibitor)
-do not use as monotherapy
Sofosbuvir
Inhibits HCV RNA-dependent RNA polymerase -> terminates chain elongation
- nucleoside analog
- do not use as monotherapy
Adenosine
rapid coronary dilation
Medication classes that should be avoided in hypertrophic cardiomyopathy (2)
- Vasodilators: Dihydropyridine calcium channel blockers, Nitroglycerine, ACE inhibitors
- Diuretics
DVT treatment in pregnancy =
Enoxaparin (LMWH)
High risk drugs for drug-induced lupus =
“Low grade fever + multiple joint pains + well demarcated erythematous rash on face and trunk + ANA positive + anti-histone positive”
- Hydralazine
- Procainamide
- Isoniazid
- Minocycline
- Quinidine
Patient who is aspirin intolerant is given _ to prevent further cardiovascular events
Clopidogrel - P2Y12 R inhibitor -> prevents platelet aggregation
Tetrodotoxin
Binds fast VG Na channels in cardiac and nerve tissue
- inactivates channels
- does not change the resting potential
Poisoning - poorly prepared puffer fish
Ciguatoxin
Main sfx
Opens VG Na channels -> depolarizaion
Temperature-related dysthesia (cold feels hot and hot feels cold) is specific
Poisoning - consumption of reef fish (barracuda, snapper, moray eel)
Scombroid poisoning
Bacterial histinide decarboxylase turns histidine -> histamine
Histamine is not degraded by heat/cooking
acute onset burning of the mouth, flushing, erythema, anaphylais-like
Scombroid poisoning treatment
anti-histamines
caused by a histamine overload
Phenylephrine
alpha1 agonist > alpha2 agonist
- increases MAP -> reflex bradycardia
- increases diastolic P
- increases systolic P
used to treat hypovolemic/distributive shock
Norepinephrine
alpha1 agonist > alpha2 agonist > beta1 agonist
- increases diastolic P
- increases systolic P
- increases MAP -> reflex bradycardia
- increases cardiac contractility
used to treat hypovolemic/distributive shock
Isoproterenol
beta1 agonist = beta2 agonist
- increases cardiac contractility
- decreases SVR
- decreases diastolic P
- decreases MAP
- increases PP
- increases HR
Dobutamine
beta1 agonist > beta2 agonist
- increases systolic P
- decreases diastolic P
- increases PP
- decreases SVR
- increases HR
- increases cardiac contractility
- increases CO
used to treat cardiogenic shock
Epinephrine
beta agonist > alpha agonist
(at low doses)
- increased cardiac contractility
- increased HR
- increased systolic P
- decreased diastolic P
- increased MAP
- decreased SVR
- increased PP
(at high doses) alpha agonist > beta agonist
Amphetamines mechanism of action
-release stored catecholamines into the synapse
Reserpine
inhibits VMAT -> neurotransmitters cannot be stored in pre-synaptic vesicles -> depletion of neurotransmitter stores
Cocaine mechanism
inhibits DAT and NET -> increased concentration of NE and dopamine in the synapse
- Clonidine
- alpha methyldopa
- tizanidine
alpha2 agonists -> decreases sympathetic outflow
beta blockers from a-m
beta1 > beta 2
“cardioselective”
beta blockers from n-z
beta1 = beta2
“nonselective”
alpha + beta blockers (2)
- Carvedilol
- Labetalol
Beers Criteria (5 main categories)
Anticholinergics:
- First generation antihistamines
- GI antispasmodics
Cardiovascular:
- Antithrombotics
- alpha blockers
- central alpha agonists
- antiarrythmics
CNS:
- TCA
- Anti-psychotics
- Barbiturates
- Benzodiazepine
Endocrine:
- Sliding scale insulins
- Sulfonylurease
Pain:
- Indomethacin
- Muscle relaxants
- Meperidine
Ranolazine
Used to treat angina refractory to other medical therapies
Mechanism: inhibits the late phase of Na current -> decreasing the diastolic wall tension and O2 consumption
No effect on HR or contractility
May prolong QT interval
MI that is treated with coronary stenting is now in recovery. Patient keeps having repeated ventricular arrhythmias caused by the ischemic tissue. What drug is given? (2)
Class IB antiarrhythmics - Lidocaine - works especially well in ischemic ventricular tissue
Class III antiarrhythmics - Amiodarone - has class I, II, III, IV activity
Antiarrhythmics that prolong QT
Class IA and Class III - Due to their effect on prolonging the ventricular action potential
This is why these classes have an increased risk for Torsades des Pointes
What antiarrhythmic drugs can be used to treat WPW?
Class IA or III antiarrhythmics
The drugs that decrease AV node conduction (II, IV) will not have an effect due to the WPW being an accessory pathway
Metolazone =
thiazide-type diuretic -> inhibits Na/Cl reabsorption in the early distal convoluted tubule
What diuretic is given to treat altitude sickness?
Acetazolamide - inhibits CA
Causes metabolic acidosis (removal of HCO3) to counteract the respiratory alkalosis that occurs at high altitudes
Bumetadine
Torsemide
Loop diuretics - inhibits Na/K/2Cl cotransporter
Also, in this class: Furosemide
Aliskiren
Direct renin inhibitor (blocks conversion of angiotensinogen to angiotensin I)
Contraindicates in patients taking ACE-I or ARBs.
oxybutamine, tolterodine, solifenacin
Reduce bladder spasms and urge incontenence
M3 antagonists -> decreases Ach activity
Guaifenesin
Expectorant - thins respiratory secretions, does not suppress cough reflex
What does N-acetylcysteine do in CF patients?
Mucolytic - loosens mucous plugs by disrupting disulfide bonds
Dextromethorphan
Antitussive
- antagonizes NMDA glutamate receptors
- synthetic codeine analog
- mild abuse potential
- may cause serotonin syndrome
Bosentan
endothelin receptor atangoinst -> decreases pulmonary vascular resistance -> vasodilation
treats pulmonary hypertenon
Epoprostenol
Iloprost
Prostacyclin analogs - PGI2
Albuterol - beta1 or beta2 agonist?
Beta2 agonist -> relaxes bronchial smooth muscle
Ipratoprium
Tiotropium
muscarinic antagonist
-used to prevent bronchoconsriction
Zileuton
5-lipoxygenase inhibitor -> decreased production of leukotrienes
Timeline of glucocorticoid function in the treatment of asthma
Takes a few weeks to work
The good thing is oral glucocorticoids do not have the same sfx profile as systemic glucocorticoids (weight gain, etc)
Side effect of albuterol for asthma treatment
Skeletal muscle tremors
Pramiprexole
Bromocriptine
Ropinirole
Dopamine receptor agonists
- First line parkinsons treatment
- Restless leg treatment
Bromocriptine - Ergot
Pramiprexole (DR-3), Ropinirole (DR-2) - Non-ergot
Amantadine
Increases dopamine release and decreases dopamine reuptake - Parkinson’s treatment for motor symptoms
Also used as an antiviral against Influenza A and Rubella
Pralidoxime
Given to patients with organophosphate poisoning to reverse the Muscarinic and Nicotinic receptor overstimulation. Only works if given early after the exposure.
Mechanism: restores cholinesterases therefore they can breakdown Ach
Baclofen
GABA-B receptor antagonist
Used in the treatment of spasticity seen in MS
Treatment and cause of Neuroleptic Malignant Syndrome
Cause: overdose of antipsychotic medications
-diffuse muscle rigidity, high fever, hypertension, tachycardia, altered sensorium, rhabdomyolysis (elevated CK)
Treatment: Dantrolene
Treatment resistant Schizophrenia is treated with
Clozapine - second generation antipsychotic
Treatment for the behavioral and psychotic manifestations of delerium?
Low dose antipsychotics (Haloperiodol)
Majority of overdose deaths in the U.S. are caused by _
Opioids - heroin and prescription analgesics
Function of methadone
- Long half life
- Mu full agonist
- Good oral bioavailability
- Suppresses withdrawal and cravings
N-methyl-D-aspartate Receptor antagonist =
PCP (Phencyclidine)
TNF-alph inhibitors - used for OA or RA treatment?
RA
Treatment for dermatomyositis or polymyositis
steroids followed by long-term immunosuppressants (methotrexate)
Inhibition of xanthine oxidase by a, increases the concentration of the active metabolite of of b.
a = allopurinol b = azathioprine
azathioprine -> 6MP -> active metabolite -> inhibition of purine synthesis
Tubocurrarine Atracurium Micacurium Pancuronium Vecuronium Rocuronium
Competitive nondepolarizing antagonist of Nicotinic R
- compete with Ach for receptors
- to reverse blockade - cholinesterase inhibitors
Depolarizing neuromuscular blocking drug (1)
Succinylcholine
- Ach R agonist -> sustained depolarization prevents muscle contraction
- Phase I - prolonged depolarization, no antidote
- Phase II - reploarized but blocked, receptors are available but desensitized, cholinesterase is antidote
- sfx: hypercalcemia, hyperkalemia, malignant hyperthermia
HLAB57O1 allele corresponds with a negative reaction to _
Abacavir - stimulates a delayed type IV hypersensitivity reaction
Why is celecoxib better than other NSAIDs?
GI protective. Does not block COX1 therefore the Gastric mucosa protection (via prostaglandins) is maintained.
Good for people who have a history of peptic ulcer disease.
What hyperlipidemia drug has the sfx of gouty arthritis?
Niacin (B3) -> decreases the renal excretion of uric acid
Main side effect of sulfonylureas? (2)
- weight gain
- hypoglycemia - dangerous in the elderly
2nd generation glyburide and glimepiride are long acting - have a higher risk for hypoglycemia
2nd generation glipizide is short acting - has a slightly less risk for hypoglycemia
Is tamoxifen used to treat a post-menopausal woman with osteoporosis?
NO
Tamoxifen is a SERM - can provide some bone protection in post-menopausal women who are also fighting ER+ breast cancer but due to its bad effects on the endometrium, it is not given as a first line osteoporosis treatment to non-breast cancer women
- antagonist in breast
- agonist in bone
- partial agonist in endometrium
What drugs can be given to treat osteoporosis in post-menopausal women? (4)
Bisphosphonates - inhibit osteoclast activity
Raloxifene - SERM
- antagonist in breast
- agonist in bone
Denosumab - RANK-L monoclonal antibody
Teraparatide - PTH analog
Patient with grave’s disease on long term antithyroid medication presents with a fever + sore throat. What is the main sfx concern?
Main SFX of thionamides (propylthiouracil/methimazole) is agranulocytosis
-absolute neutrophil count is less than 500
Oral fidaxomicin
recurrent cases of C. diff infections
part of the macrolide family
Sulfasalazine
Combination drug of sulfapyridine (antibacterial) + 5-aminosalicylic acid (anti-inflammatory)
First line for ulcerative colitis
Arsenic poisoning/overload treatment?
Dimercaprol chelation
Carcinoid treatment
- Octreotide - somatostatin analog
- Surgery
Treatment of lyme disease in pregnancy
Amoxicillin
Normal (non-pregnancy) treatment of Lyme Disease is doxycycline but this has teratogenic effects (teeth staining)
Mifepristone (RU-486)
- progesterone antagonist (->necrosis of the uterine decidua)
- glucocorticoid antagonist
Flutamide
competitive inhibitor at androgen receptors
used in the treatment of prostate cancer
Minodixil
Direct arteriolar vasodilator
Used for androgenic alopecia or severe refractory HTN
sfx: sympathetic activation and RAAS activation
Clot busting of an ST elevated MI
Fibrinolytic drugs - useful if given within 6 hours of onset
Two classes fibrin specific (attacks fibrin that is attached to a clot only) or non-fibrin specific (ex: Streptokinase)
SFX: may cause re-perfusion arrhythmia but these are usually benign
Argatroban
Lepirudin
Hirudin
Direct thrombin inhibitors (Factor II)
-Used to treat Heparin Induced Thrombocytopenia
Rasburicase
recombinant version of urate oxidase
(uric acid -> allantoin)
given to help prevent the hyperuricemia of tumor lysis syndrome
Antidote for cyanide poisoning
Inhaled amyl/sodium nitrite
Cyanide inhibits cytochrome c oxidase in the ETC.
Amyl nitrite oxidizes Hb Fe2+ -> Fe3+ (methemoglobin) which has a high affinity for cyanide and can bind it up so that the cyanide cannot bind to the ETC.
Triptans
- mechanism
- contraindications
serotonin (5HT 1b/1d) agonists)
- inhibit release of vasoactive peptides
- promote vasoconstriction
- block pain pathways in brainstem
should be avoided in patients with cardiac or cerebrovascular disease
Nitroprusside toxicity
Cyanide poisoning leading to sulfur depletion
- CN -> (-) ETC cytochrome oxidase
- altered mental status, seizures, cardovascular collapse, lactic acidosis, bright red blood
- CN metabolism occurs by transferring a sulfur group onto it
- Eventually sulfur stores are depleted, give sodium thiosulfate for antidote
Valproate teratogenicity
neural tube defects
Ramelteon
melatonin receptor agonist
- safe in older adults
- few side effects
- melatonin receptors are in the chiasmatic nucleus
Phenylephrine
Xylometazoline
Oxymetazoline
topical treatment of allergic rhinitis
alpha-agonists
Flumazenil
Antidote for Benzodiazepine, Nonbenzodiazepine hypnotic overdose
- competitive antagonist at GABA benzodiazepine receptor
- may precipitate seizures
Beta blocker overdose treatment?
Glucagon
Copper, Arsenic, Gold OD treatment?
Penacillamine
Methemoglobin toxicity treatment
Methylene blue, Vitamin C
Salicylates toxicity treatment
NaHCO3 + dialysis
-alkalinizes the urine
Aminocaproic acid is used for?
tPA, Streptokinase, Urokinase reversal
Warfarin reversal?
- Vitamin K - delayed effect
- Fresh frozen plasma - immediate
Timolol acts where when treating open-angle glaucoma?
Acts on the the ciliary epithelium.
- nonselective beta-blocker
- decreases aqueous humor production
Acetazolamide works via what mechanism to treat open-angle glaucoma?
Decreases aqueous humor production from the ciliary epithelium
Lantanoprost, Travoprost work via what mechanism to treat open-angle glaucoma?
Prostaglandin agonists (PG2-alpha)
Increase aqueous humor outflow and therefore decreases intraocular pressure
Pilocarpine, Carbachol work via what mechanism to treat open-angle glaucoma?
(direct) Cholinomemetics
Increase aqueous humor outflow via contraction of ciliar muscles and opening of trabecular meshwork, therefore decreases intraocular pressure
sfx: miosis, cyclospasm
Brimonidine’s mechanisim for treatment of open-angle glaucoma
alpha-2 agonist
-acts at ciliary body - decreases aqueous humor synthesis
IL-2 can be used as treatment for what 2 cancers?
- Renal cell carcinoma
- Melanoma
Infliximab
- chimeric human/mouse antibody to TNF-alpha
- used in treatment of RA, ankylosing spondylitis, Crohn’s disease
- anti-TNF-alpha
Gabapentin
Inhibits (active) VG Ca channels
- GABA analogue
- used to treat painful diabetic neuropathy, fibromyalgia, post-herpetic neuralgia, simple seizures
- sfx: ataxia, confusion
First line treatment for trigeminal neuralgia
Carbamazepine = increaes Na channel inactivation
-sfx: myelosuppression/agranulocytosis
Etanercept
recombinant TNF receptor fusion protein (anti-TNF-alpha)
How does lactulose work?
acidifies the contents of the GI tract -> NH3 diffuses into GI and turns into NH4+ and now gets trapped
Mechanism: Inhibition of peptidoglycan synthesis via the blockade of transpeptidation enzymes
Use: to prevent PID
What drug?
Ceftriaxone
transpeptidation enzymes = PBPs
Cyclosporine
Calcineurin inhibitor - blocks IL-2 transcription
- binds to cyclophilin
- used for transplant rejection prophylaxis, psoriasis, RA
- sfx: nephrotoxic (dose dependent)
Tacrolimus (FK506)
Calcineurin inhibitor - blocks IL-2 transcription
- binds to FKBP
- used for transplant rejection prophylaxis
- sfx: nephrotoxic
Metoclopramide
mechanism?
contraindications?
D2 receptor antagonist
- prokinetic agent, does not influence colonic transport time
- contraindicated in parkison’s patients or patients with small bowel obstruction
Calcipotriol
Vitamin D analog used to treat psoriasis
-topical
Acitretin
Retinoid
- used to treat psoriasis, acne, photoaging, some skin neoplasms
- this is preferred for psoriasis
- teratogenic - should not conceive for up to 3 years after stopping
Orlistat
Inhibits pancreatic and gastric lipase -> decreases breakdown and absorption of dietary fats
Used for weightloss
sfx: diarrhea, steatorrhea,
danazol
androgen used to suppress FSH and LH release by the pituitary
Treatment of sexual dysfunction caused by mumps induced orchitis
Testosterone
orchitis -> leydig cell atrophy -> decreased production of T -> sexual dysfunction
Paclitaxel coated stent does what?
causes cell cycle arrest in the M phase -> inhibits cellular division -> prevents stent re-stenosis by preventing intimal hyperplasia
patient on furosemide who experiences excessive urination and occasional weakness and cramps
Furosemide sfx
- increased dilute urine production
- hypokalemia (and contraction metabolic alkalosis)
Vemurafenib
BRAF kinase inhibitor
- used to treat metastatic or unresectable melanoma
- specific for BRAF V600E
direct arterial vasodilators (2)
-sfx
- Hydralazine
- Minodixil
sfx:
-reflex sympathetic and RAAS activation -> increases Na and fluid retention
