Pharmacology Flashcards
How does one calculate: 1. Volume of distribution 2. Clearance 3. Loading dose 4. Maintenance dose >> MUST KNOW EQUATIONS
Vd = D/C
- Vd = Volume of distribution
- D = Amount of drug in IV form (100% bioavailability)
- C: Concentration of drug in plasma
CL = 0.7/0.5t x Vd = rate of elimination of drug/plasma concentration of the drug
- CL = Clearance
- 0.5t = 1/2t = half-life of the drug
LD = Css x Vd
- LD = Loading Dose
- Css = Concentration at steady state = Desired/Target concentration of the drug
MD = Css x CL
- MD = Maintenance Dose
What is efficacy (of a drug)?
The maximal effect a drug can produce
What is potency (of a drug)?
The amount of drug needed for a given effect
What drug inhibits the transport of choline into the presynaptic cell?
Hemicholinium
What drug inhibits the packaging of acetylcholine into vesicles in the presynaptic cell?
Vesamicole
What enzyme catalyzes the production of acetylcholine from choline and acetyl-CoA?
Choline acetyltransferase
What toxin further stimulates acetylcholine presynpatic release, and what kind of paralysis does it cause?
Black widow spider toxin
- Spastic paralysis
What toxin inhibits acetycholine presynpatic release, and what kind of paralysis does it cause?
Botulinum toxin
- Flaccid paralysis
Describe the catecholamine synthesis pathway.
Phenylalanine —–> Tyrosine (phenylalanine hydroxylase)
Tyrosine ——> DOPA (tyrosine hydroxylase)
DOPA ——> Dopamine (DOPA carboxylase + B6)
Dopamine ——> Norepinephrine (requires vit. C)
Norepinephrine ——-> Epinephrine
What drug inhibits tyrosine hydroxylase?
Metyrosine
What drug inhibits the packaging of norepinephrine vesicles?
Reserpine
What drugs further stimulate the release of norepinephrine from the presynaptic cell?
- Calcium
- Amphetamines
- Ephedrine
- Tyramine
What drugs inhibit the release of norepinephrine from the presynaptic cell?
- Guanethidine
- Bretylium
What drugs inhibit the reuptake of norepinephrine into the presynaptic cell?
- Cocaine
- Tricyclic antidepressants
What are the enzymes responsible for metabolism of catecholamines?
- COMT (methylation of NE)
- MAO (oxidation of NE)
Which receptors are Gq-protein-linked receptors?
Cutsies HAVe 1 M&M.
- Histamine 1 receptor
- Alpha-1 adrenergic receptor
- Vasopressin V1 receptor
- Muscarinic 1 M1 receptor
- Muscarinic 3 M3 receptor
Which receptors are Gi-protein-linked receptors?
MAD2
- Muscarinic M2 receptor
- Alpha-2 adrenergic receptor
- Dopamine D2 receptor
Which receptors are Gs-protein-linked receptors?
- Beta-1 adrenergic receptor
- Beta-2 adrenergic receptor
- Dopamine D1 receptor
- Histamine H2 receptor
- Vasopressin V2 receptor
Put the following in their respective categories of:
(A) Direct cholinergic agonists
(B) Indirect cholinergic agonists
(C) Anti-muscarinic/anti-cholinergic drugs
(D) Direct sympathomimetics
(E) Indirect sympathomimetics
(F) Alpha blockers: selective VS. nonselective
(G) Beta blockers
Phentolamine, prazosin, terazosin, homatropine, acebutolol, rivastigmine, bethanechol, propranolol, timolol, physostigmine, nadolol, norepinephrine, albuterol, clonidine, ephedrine, carvedilol, darifenacin, atenolol, echothiophate, atropine, tropicamide, benztropine, tamsulosin, dobutamine, pilocarpine, epinephrine, esmolol, methacholine, neostigmine, a-methyldopa, mirtazapine, tolterodine, ipratropium, glycopyrrolate, carbachol, donepezil, galantamine, salmeterol, pyridostigmine, labetalol, solifenacin, cocaine, pindolol, trospium, dopamine, isoproterenol, oxybutynin, edrophonium, terbutaline, amphetamine, phenoxybenzamine, phenylephrine, doxazosin, metoprolol, scopolamine, tiotropium
Direct cholinergic agonists
- Bethanechol
- Pilocarpine
- Methacholine
- Carbachol
Indirect cholinergic agonists
- Neostigmine
- Pyridostigmine
- Edrophonium
- Physostigmine
- Echothiophate
- Donezepil
- Galantamine
- Rivastigmine
Anti-muscarinics
- Atropine
- Homatropine
- Tropicamide
- Benztropine
- Scopolamine
- Ipratropium
- Tiotropium
- Glycopyrrolate
- Oxybutynin
- Tolterodine
- Darifenacin
- Solifenacin
- Trospium
Direct sympathomimetics
- Epinephrine (a1, a2, b1, b2)
- Norepinephrine (a1, a2, b1)
- Dopamine (D1, D2 >> b1, b2 >> a1, a2)
- Dobutamine (b1)
- Isoproterenol (b1, b2)
- Phenylephrine (a1)
- Albuterol (b2)
- Salmeterol (b2)
- Terbutaline (b2)
- Clonidine (a2)
- a-methyldopa (a2)
Indirect sympathomimetics
- Ephedrine
- Cocaine
- Amphetamine
Alpha blockers
- Nonselective: phentolamine, phenoxybenzamine
- Selective: prazosin, terazosin, doxazosin, tamsulosin
- a2-selective: mirtazapine
Beta-blockers
- Non-selective: propranolol, timolol, nadolol
- Beta-1 selective: atenolol, esmolol, metoprolol
- Beta-1 and alpha-1 selective: carvedilol, labetalol
- Weak beta-1 and beta-2 agonists: acebutolol, pindolol
Antidote and treatment: acetaminophen
N-acetylcysteine
Antidote and treatment: AChE inhibitors overdose/organophosphate poisoning
- Atropine
- Pralidoxime
Antidote and treatment: amphetamine
- NH4CL
- Benzodiazepines
- Antipsychotics
- Antihypertensives
Antidote and treatment: antimuscarinics
Physostigmine salicylate
Antidote and treatment: benzodiazepines
- Flumazenil
Antidote and treatment: B-blockers
- Glucagon
- Atropine
- Calcium
Antidote and treatment: carbon monoxide
- 100% oxygen
- Hyperbaric oxygen
Antidote and treatment: copper, arsenic and gold
- Penicillamine
Antidote and treatment: cyanide
- Thiosulfate + nitrite
- Hydroxocobalamin
Antidote and treatment: digitalis/digoxin
- Potassium and magnesium balance
- Anti-dig Fab fragments
Antidote and treatment: heparin
- Protamine sulfate
Antidote and treatment: iron
- Deferoxamine
- Deferasirox
Antidote and treatment: lead
- EDTA
- Dimercaprol
- Succimer
- Penicillamine
Antidote and treatment: mercury, arsenic, gold
- Dimercaprol
- Succimer
Antidote and treatment: methanol, ethylene glycol
- Fomepizole
- Ethanol
- Dialysis
Antidote and treatment: methemoglobin
- Methylene blue
- Vitamin C
Antidote and treatment: Opioids
- Naloxone
- Naltrexone
Antidote and treatment: salicylates
- NaHCO3
Antidote and treatment: TCAs
- NaHCO3
Antidote and treatment: tPA, streptokinase, urokinase
- Aminocaproic acid
Antidote and treatment: warfarin
- Vitamin K
- Fresh frozen plasma
Antidote and treatment: theophylline
- B-blockers
What drugs (other than muscarinic antagonists themselves) have anticholinergic effects?
- First generation H1R antagonist
>> Diphenhydramine
>> Chlorpheniramine - Neuroleptics
>> Thioridazine
>> Chlorpromazine
>> Olanzapine
>> Clozapine - Tricyclic antidepressants
- Amantadine
What drugs can cause agranulocytosis?
4Cs and 1D
- Clozapine
- Carbamazepine
- Colchicine
- Carbimazole/methimazole and PTU
- Dapsone
What drugs can cause aplastic anemia?
Can’t Make New Blood Cells Properly
- Carbamazepine
- Methimazole
- NSAIDs
- Benzene
- Chloramphenicol
- Propiothiouracil (PTU)
What drugs can cause megaloblastic anemia?
Have a blast with PMS.
- Phenytoin
- Methotrexate
- Sulfa drugs
