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