Pharmacology Flashcards
What are the functions of the α2 receptor?
Decrease in sympathetic outflow
Decrease in insulin release
Decrease in lipolysis
Increase in platelet aggregation
What are the functions of the β1 receptor?
Increased heart rate
Increased contractility
Increased renin release
Increased lipolysis
What are the functions of the β2 receptors?
Vasodilation, bronchodilation
Increased heart rate
Increased contractility
Increased lipolysis, increased insulin release
Decreased uterine tone, ciliary muscle relaxation
Increased aqueous humor production
What are the functions of the M1 receptor?
CNS, enteric nervous system activation
What are the functions of the M2 receptor?
Decreased heart rate and contractility of atria
What are the functions of the M3 receptor?
Increased exocrine gland secretions
Increased gut peristalsis
Increased bladder contraction, bronchoconstriction
Increased pupillary sphincter muscle contraction (miosis)
Ciliary muscle contraction (accommodation)
What is the major function of the D1 receptor?
Relaxes renal vascular smooth muscle
What is the major function of the D2 receptor?
Modulates transmitter release, especially in the brain
What are the functions of the H1 receptor?
Increased nasal and bronchial mucus production
Increased vascular permeability
Contraction of bronchioles, pruritis, and pain
What is the major function of the H2 receptor?
Increased gastric acid secretion
What is the major function of the V1 receptor (vasopressin)?
Increased vascular smooth muscle contraction
What is the major function of the V2 receptor?
Increased H2O permeability and reabsorption in the collecting tubules of the kidney
What is associated with cholinesterase inhibitor poisoning (DUMBBELSS)?
Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation (of skeletal muscle and CNS) Lacrimation Sweating Salivation
What is associated with Atropine (Muscarinic antagonist) toxicity?
Hot as a hare Dry as a bone Red as a beet (flushed skin) Blind as a bat (cycloplegia) Mad as a hatter
Why does norepinephrine (α1>α2>β1) cause bradycardia?
Reflex bradycardia due to increased blood pressure
What is the difference between the α blockers Phenoxybenzamine and phentolamine?
Phenoxybenzamine is irreversible
What is the effect of an alpha blocker on blood pressure responses to epinephrine (β>α) and phenylephrine (α1>α2)?
The epinephrine response exhibits reversal of the mean blood pressure change, from a net increase (the α response) to a net decrease (the β2 response). The response to phenylephrine is suppressed but not reversed because phenylephrine is a “pure” α agonist without β action
β1 selective agonists go mostly from _ to _ (in the alphabet)
A-M
Acebutolol (partial), Atenolol, Betaxolol, Esmolol, Metoprolol
Non-selective β antagonists mostly go from _ to _ (in the alphabet)
N-Z
Nadolol, pindolol (partial), Propanolol, Timolol
What is administered with cyclophosphamide to prevent hemorrhagic cystitis?
Mesna
What are the sulfa drugs? (Popular FACTSSS)
Probenecid Furosemide Acetazolamide Celecoxib Thiazides Sulfonamide antibiotics Sulfasalazine Sulfonylureas
What are the functions of the α1 receptor?
Increase in vascular smooth muscle contraction
Increase in pupillary dilator muscle contraction
Increase in intestinal and bladder sphincter muscle contraction
What are the CYP450 inducers?
Carbamazepine Barbiturates Phenytoin Rifampin Griseofulvin "Guinness, Coronas, and PBRs induce chronic alcoholism"
What are the CYP 450 Inhibitors?
Cimetidine Ciprofloxacine Erythromycin Azole antifungals Grapefruit juicce Isoniazid Ritonavir (protease inhibitors)
Which drugs have anticholinergic side effects?
Typical neuroleptics: Thioridazine, chlorpromazine
1st generation antihistamines: Diphenhydramine, hydroxyzine
TCAs: Amitriptyline
Amantadine
Which drugs are eliminated with zero-order elimination?
Phenytoin
Ethanol
Asprin
“A PEA is round like zero”
On a lineweaver-Burk plot, what is the X axis? What is the Y axis?
X axis: 1/[S]
Y axis: 1/[V]
On a Lineweaver-Burk Plot, what is represented by the point where the line crosses the y axis? the x axis? What is represented by the slope?
Crosses Y axis: 1/Vmax
Crosses X axis: 1/(-Km)
Slope: Km/Vmax
A drug infused at a constant rate takes _ - _ half lives to reach steady state
___ half lives to reach 90% of the steady state
4-5
3.3
What is the equation for loading dose of a drug?
Loading dose = (Cp x Vd)/F
Cp = target plasma concentration at steady state F = bioavilability
What is the equation for maintenance dose?
Maintenance dose = (Cp x CL x t)/F
Cp = target plasma concentration at steady state CL = clearance t = dosage interval (time between doses)
Nicotinic ACh receptors are ligand gated ________ channels
Muscarinic ACh receptors are ________ _______ receptors
Nicotinic ACh receptors are ligand gated Na+/K+ channels
Muscarinic ACh receptors are G-protein coupled receptors
What drug is given for atropine overdose?
Physostigmine
What was previously used for the diagnosis of MG? What is used now?
Previously: Edrophonium (anticholinesterase)
Now: AChR Ab (anti-acetylcholine receptor antibody) test
What is the antidote for cholinesterase inhibitor poisoning?
Atropine
What are the effects of dopamine at low doses? High doses?
Dopamine (D1=D2 > β > α)
Used for unstable bradycardia, heart failure, and shock at low/middle doses
Inotropic and chronotropic α effects predominate at high doses
Why do you never give β blockers when cocaine intoxication is suspected?
Can lead to unopposed α1 activation and extreme hypertension
What are the α2 sympatholytics (agonists) - when are they used
Clonidine - hypertensive urgency (does not decrease renal blood flow)
α-methyldopa - hypertension in pregnancy
What α blocker do you give to MAO inhibitors who eat tyramine containing foods?
Phentolamine (reversible)
How do Beta blockers affect glaucoma?
Decrease secretion of aqueous humor (timolol)
How is β blocker overdose treated?
Glucagon
How is methanol/ethylene glycol overdose treated?
Fomepizole
What drugs can cause focal to massive hepatic necrosis (HAVAc)
Halothane
Amanita phalloides
Valproate
Acetaminophen
Which drugs redistribute to fat? (Fat PiG)
Protease inhibitors, Glucocorticoids
