Pharmacology - Targets/Mechanism Flashcards
Abciximab
A-B-ciximab - gp2B3A
gp2b/3a receptor
monoclonal antibody to gp2b3a - prevent platelets binding fibrinogen
[Eptifibatide, Tirofiban]
Acetaminophen
weak cyclooxygenase inhibitor… CNS?
Acetazolamide
Carbonic Anhydrase inhibitor - inhibits CA in proximal tubule, causes NaHCO3 diuresis –> bicarb depletion and metabolic acidosis
[Dorzolamide, Brinzolamde; topical analogues]
Acetylcholine
Cholinomimetic prototype; neurotransmitter
Acyclovir
Inhibits DNA synthesis in HSV and VZV; requires viral thymidine kinase
[Famciclovir, Penciclovir, Valacyclovir]
Adenosine
Antiarrhythmic; hyperpolarizes AV node (via adenosine specific Gi that decreases cAMP and increases K outflow), blocks conduction for 10-15s
Rx; Best at reentrant circuits
Albuterol
B2 agonist, rapid-acting
[Metaproterenol, Terbutaline]
Alendronate
Bisphosphonate (Rx: osteoporosis, hypercalcemia)
Complex: act on hydroxyapatite crystal structure of bone, effects on vit D production and Ca absorption, and direct effect on osteoclasts
[Etidronate, Pamidronate, Risedronate]
Allopurinol
Irreversible inhibitor of xanthine oxidase; reduces production of uric acid
[Febuxostat]
Rx; Gout, especially used chronic gout
Alteplase
t-PA
Thrombolytic; recombinant tissue plasminogen activator
[Reteplase, Tenecteplase]
Amiloride
K-sparing diuretic; blocks epithelial Na channels (ENaC) in cortical collecting tubules
Amiodarone
Group 3 antiarrhythmic
unique: blocks sodium, potassium, CALCIUM, and beta receptors
Ampicillin
Beta-lactam, Penicillin-binding protein
Prevents cross-linking of peptidoglycan cell wall (stage III synthesis)
[Amoxicillin]
Anastrozole
Aromatase inhibitor
inhibits conversion of Testosterone to Estradiol (in adipocytes)
[Letrozole]
-Used for ER positive breast cancer
Aspirin
irreversible COX-1 and COX-2 inhibitor
9x greater affinity for platelet enzyme that makes TXA2 over endothelial cell enzymes
Atenolol
Selective B1 Blocker
Atropine
Non-selective Muscarinic Blocker; competitive inhibitor at M1, M2, M3
Azithromycin
Macrolide ABx
Bind ribosomal 50S and block transpeptidation (prevents charged tRNA [tRNA+a.a.] from passing its a.a. to the growing polypeptide chain, thus halting translation)
Macrolide - no slide
Baclofen
GABA analog
-Used for spasticity
Benztropine
like Atropine
Non selective, competitive Anti-muscarinic
Rx for Parkinsonism
Botulinum
Toxin (Clostriudium botulinum)
cleave synaptotagmin, synaptobrevin, SNARE proteins, prevents acetylcholine vesicle release
Bromocriptine
dopamine agonist in CNS (more D2 specific)
**Cabergoline is now more commonly used
Rx; parkinson’s, Prolactinoma
Bupivacaine
local anesthetic, long-acting amide
Sodium channel blocker, prevents depolarization
non-ionized form diffuses into cell, ionized form blocks channel
use-dependent
Buprenorphine
opioid
long-acting partial agonist of mu receptor
Bupropion
Mechanism unknown
Go Fuck Yourself, Sam
Rx; depression, smoking cessation, seasonal affective disorder
Captopril
ACE Inhibitor
Angiotensin Converting Enzyme Inhibitor - decreases angiotensin II and aldosterone, increases kinin family (bradykinin) vasodilators
[Benazepril, Enalapril, Lisinopril, Quinapril]
Carbamazepine
Anti-seizure
Blocks Na channels in neuronal membranes
Carvedilol
Non-selective adrenoblocker
racemic mix; one isomer blocks B1 & B2 non-selectively, the other isomer blocks A1
[Labetalol]
Sam loves touching Clay’s nuts
Caspofungin
echinocandin prototype
inhibitor of Beta(1-3)-glucan synthesis, cell wall component
Cefazolin
First Gen Cephalosporin
(Get your phd to first, but don’t be FAZed by ceFAZolin)
beta-lactam, inhibitor of peptidoglycan cross-linking, cell wall synthesis
Ceftriaxone
Third Gen Cephalosporin
(Third generations have T in the name)
Beta-lactam, inhibit peptidoglycan cross-linking
[Cefotaxime, Ceftazidime]
Celecoxib
Selective COX-2 In’bitor
Chloramphenicol
Broad Spectrum ABx
inhibits 50s bacterial ribosome
Chloroquine
Antimalarial
Binds to hemin, causing dysfunctional cell membranes
Chlorpheniramine
Antihistamine first generation H1 blocker
[Diphenhydramine]
Chlorpromazine
Phenothiazine antipsychotic
Blocks dopamine receptors in CNS
[Fluphenazine, Trifluoperazine]
Cholestyramine
Antihyperlipidemic
bile acid binding resin sequesters bile acids in GI and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins
[Colestipol, Colesevelam]
Cimetidine
H2 Blocker on gastric parietal cells
ECL cells in gastric mucosa secrete Histamine which binds to H2 receptors on Parietal Cells. H2 are Gs, increase Parietal intracellular cAMP, which stimulates H/K-ATPase to secrete H into stomach lumen.
[Ranitidine, Famotidine, Nizatidine]
Ciprofloxacin
Second Generation Fluoroquinolone
Bactericidal Inhibitor of DNA gyrase
Cisplatin
Antineoplastic - CCNS (Cell cycle non-specific)
platinum containing alkylating anticancer drug active against solid tumors (e.g. testes, lung)
Adds alkyls to DNA bases (esp. N7 of Guanine), causing abnormal cross-linking and DNA strand breakage.
[Carboplatin, Oxaliplatin]
Clindamycin
Lincosamide antibiotic
Bacteriostatic 50s ribosomal inhibitor
Clomiphene
SERM - selective estrogen receptor modulator
Blocks pituitary estrogen receptors to induce ovulation
Clonidine
Centrally Acting Alpha2 agonist
reduces Sympathetic outflow (SANS) and lowers BP
[Methyldopa]
Clopidogrel
Antiplatelet
Irreversibly inhibits platelet ADP receptors, prevents expression of gp2a/3b receptors which bind fibrinogen
[Ticlopidine]
Cocaine
Indirect sympathomimetic
Inhibits norepinephrine transporter (NET) in the presynaptic membrane, increasing synaptic activity of NE
[Tricyclic antidepressents act in the same way, also inhibiting dopamine transporter, DAT]
Colchicine
Microtubule assembly inhibitor
Reduces macrophage mobility and phagocytosis
(Rx: chronic gout)
Cyclophosphamide
Antineoplastic, immunosuppressive
Cell Cycle Nonspecific (CCNS) alkylating agent (adds alkyls to DNA bases, causing cross-linking and strand breaks)
Cyclosporine
Immunosuppressant
immunophilin ligand
Prevents cytokine production by activated T-Cells; binds to cyclophilin, this complex inhibits calcineurin which regulates nuclear factor of activated T cells (NF-AT), a transcription factor which translocates to the nucleus to increase production of cytokines IL-2, IL-3, & IFNgamma
[Tacrolimus, similar, binds FKBP instead of cyclophilin]
Dantrolene
Blocks Ca++ release from sarcoplasmic reticulum of skeletal muscle
Emergent Rx: Malignant hyperthermia
Desmopressin
Vasopressin (ADH) analogue
more selective for V2 receptors
[Vasopressin]
V1: Gq - increase vascular sm contraction
V2: Gs - increase H2O perm in collecting tubule
(V2 in 2 kidneys)
Diazepam
benzodiazepam prototype
binds BZ receptros of the GABAa receptor-chloride ion channel complex
facilitates the inhibitory actions of GABA by increasing the FREQUENCY of channel opening
[Alprazolam, Lorazepam, Midazolam]
Digoxin
positive inotropic glycoside prototype
Inhibits Na/K-ATPase, increasing intracellular Na, which reverses the Na/Ca Exchanger, ultimately increasing intracellular Ca++ –> increased contractility
Diphenhydramine
Antihistamine
H1-Blocker
[Doxylamine]
Dopamine
Neurotransmitter, agonist at dopamine receptor
D1: Gs, relaxes vascular smooth muscle
D2: Gi, modulates neurotransmitter release esp. in brain
Doxorubicin
Antineoplastic
Anthracycline drug (Cell-Cycle Nonspecific)
intercalates between base pairs to disrupt DNA function, inhibits topoisomerases, forms cytotoxic free radicals
[Daunorubicin]
Doxycycline
Tetracycline
Bacteriostatic 30s ribosomal protein synthesis inhibitor
Edrophonium
Cholinesterase inhibitor
Prevents degradation of acetylcholine by inhibiting cholinesterase, used for myasthenia gravis diagnosis
Efavirenz
NNRTI (Nonnucleoside Reverse Transcriptase Inhibitor)
[Delavirdine, Nevirapine]
Enfuvirtide
Antiviral
HIV fusion inhibitor
synthetic peptide that binds HIV gp41 subunit of the viral envelope, preventing conformational changes required for fusion
Enoxaparin
Low Molecular Weight Heparin
activity against Factor Xa
[dalteparin, tinzaparin]
Entacapone
COMT inhibitor (Catechol-O-methyltransferase) Acts in the periphery only, prevents conversion of levodopa to 3-O-methyldopa; 3OMD competes with levodopa for transport into CNS and thus decreases effectiveness of levodopa. COMT inhibitors increase CNS levels of levodopa [Tolcapone]
Ephedrine
Indirect sympathomimetic
Displaces stored catecholamines
Like amphetamine but with less CNS stimulation and more smooth muscle effects
Epinephrine
Adrenoreceptor agonist
product of adrenal medulla
affinity for all alpha and beta receptors
Ergot alkaloids
ergotamine
prolonged vasoconstriction and uterine contraction
[Ergonovine, ergotamine]
Erythromycin
Macrolide - No slide - macrolide
bacteriostatic protein synthesis inhibitor at 50s
[Azithromycin, clarithromycin]
Etanercept
DMARD (disease modifying anti-rheumatic drug)
Immunoglobulin based recombinant protein that binds to and inhibits TNFalpha
[Infliximab, adalimumab]
Ethambutol
Antimycobacterial
inhibitor of arabinogalactan synthesis, a cell wall component, commonly standard part of TB Rx
Ethosuximide
Anticonvulsant
may block T type Ca channels in thalamic neurons
Rx Absence seizures
Ezetimibe
Antihyperlipidemic (EZetimibe-EZglide)
inhibits GI transporter of dietary cholesterol and the cholesterol secreted in bile, inhibits cholesterol uptake in GI
Fentanyl
Short-acting opiod agonist
[Remifentanil, sufentanil]
Finasteride
Antiandrogen
Steroid inhibitor of 5alpha-reductase that in hibits sythesis of dihydrotestosterone (DHT)
[Dutasteride]
Fleicanide
Group 1C antiarrhythmic
use and state-dependent Na Channel blocker, no effect on action potential duration of QT interval
Slow conduction velocity and pacemaker activity
Fluconazole
Imidazole antifungal
inhibits ergosterol synthesis, thereby interfering with fungal cell wall permeability
Fludrocortisone
Synthetic corticosteroid High mineralocorticoid (Na retention, K/H wasting), moderate glucocorticoid activity (increase glucose and insulin, catabolize proteins, suppress cellular immunity, antiinflammatory cytokines) steroid transported bound to protein, diffuses into cell, binds cytosolic receptor, translocates to nucleus and stimulates tissue-specific gene expression
Flumazenil
Benzodiazepam receptor antagonist
Fluorouracil
Antineoplastic, Cell-Cycle Specific (CCS)
pyrimidine antimetabolite
irreversibly inhibits thymidylate synthase, resulting in dTMP deficiency and a “thymine-less” cell death
(uracil is a base, think of deficiency of another base, thymine)
Fluoxetine
SSRI antidepressent
Selective Serotonin Reuptake Inhibitor
[citalopram, escitalopram, fluvoxamine, paroxetine, sertraline]
Flutamide
Antiandrogen
Androgen receptor antagonist for Prostate Cancer
[biclutamide, nilutamide]
Furosemide
Loop diuretic
Inhibits Na/K/2Cl transporter in the thick ascending loop
Gabapentin
Anticonvulsant
analog of GABA, facilitates the inhibitory action in the CNS
Rx partial seizures, bipolar, neuropathic pain
Ganciclovir
Antiviral
triphosphorylated guanine derivative that causes chain termination (acts at level of DNA polymerase)
Gemfibrozil
Antihyperlipidemic:
Fibrate class
Activates peroxisome proliferator-activated receptor-alpha (PPARa), a gene regulator, which enhances triglyceride clearance by increasing synthesis of lipoprotein lipase in endothelial cells. In the liver it stimulates fatty acid oxidation (uses them up) which decreases VLDL, and increase apoA1 and A2 production, increasing HDL.
Lowers Triglycerides and VLDL, increases HDL.
Gentamicin
Aminoglycoside
Bacterocidal 30s inhibitor
[Tobramycin]
Glipizide
Antidiabetic (GLipizide–GLUCOSE)
potent sulfonylrea secretagogue
Blocks K channels in pancreatic Beta cells, depolarizing them, causing calcium induced fusion of vesicles and secretion of insulin
[Glyburide, repaglinide]
Glucagon
Hormone
From pancreatic Alpha cells
Increases blood glucose via increased cAMP
Haloperidol
Antipsychotic butyrophenone
blocks brain D2 receptors
Halothane
General Anesthetic
volatile (inhaled) halogenated hydrocarbon
[isoflurane, sevoflurane]
Heparin
Anticoagulant
large polymeric molecule with activity against thrombin and factor X
Antidote: protamine
Hydralazine
Antihypertensive
arteriolar vasodilator
Causes release of endothelial NO which diffuses into smooth muscle cells and stimulates Guanylyl Cyclase to make cGMP, which dephosphorylates Myosin-LC-PO4 to Myosin-LC –> relaxation
[Minoxidil]
Hydrochlorothiazide
Thiazide diuretic
blocks Na/Cl transporter in Distal Convoluted Tubule, also stimulates uptake of Ca++
Hydroxychloroquine
DMARD (disease modifying anti rheumatic drug)
antimalarial and T-cell immunosuppressent for rheumatoid arthritis
[methotrexate, sulfasalazine]
Ibuprofen
NSAID
nonselective COX inhibitor with analgesic, antipyretic, and anti inflammatory actions similar to ASA
Imipenem
Carbapenem ABx prototype
Bactericidal inhibitor of cell wall synthesis
[meropenem, ertapenem]
Imipramine
Tricyclic antidepressent Blocks the reuptake of 5-HT and NE Similar to SNRIs but with broader peripheral effects (SNRIs are more selective) [amitriptyline, clomipramine, doxepin]
Indinavir
Antiviral
HIV protease inhibitor
Inhibits the protease which is essential for cleaving HIV proteins into proper length/configuration
[amprenavir, nelfinavir, ritonavir, saquinavir]
Indomethacin
Highly potent NSAID
Rx for neonatal PDA or acute inflammatory rxn (e.g. gout)
Ipratropium
Antimuscarinic
aerosol for asthma
competitively block muscarinic receptors in the airway, effectively preventing bronchoconstriction from vagal discharge
[Tiotropium]
Isoniazid
antimycobacterial
structurally similar to pyridoxine (vit B6)
Mechanism involves inhibition of mycolic acid, a characteristic component of mycobacterial cell walls.
Must be activated by a tubercular enzyme, and then targets a different enzyme, thus there is double opportunity for resistance.
Isoproterenol
Beta agonist, B1 & B2
Bronchodilator, cardiac stimulant
Ivermectin
Antihelminthic
intensifies GABA mediated neurotransmission in nematodes, no access to human CNS
Ketoconazole
Antifungal azole prototype
Inhibits synthesis of ergosterol
interferes with fungal cell membrane permeability by preventing ergosterol synthesis, acting at the step of 14alpha-demethylation of lanosterol
[fluconazole, itraconazole, voriconazole]
Ketorolac
NSAID
mainly used as a systemic analgesic
Lamivudine
3TC
Nucleoside reverse transcriptase inhibitor (NRTI)
Triphosphorylated nucleoside that competitively inhibits binding of dNTP-binding site of reverse transcriptase AND cause chain terminators via insertion into growing DNA chain
Lamotrigine
Antiepileptic
rate-dependent Na channel blocker, prolongs the inactivated state of Na channel, increasing refractory period of neuron
Absence and partial seizures
Latanoprost
Prostaglandin F, topically for closed angle glaucoma
Lepirudin
Direct thrombin inhibitor
recombinant form of medicinal leech protein, directly inhibits thrombin
(LEpirudin –> LEECH)
Leuprolide
GnRH analog
continuous therapy down regulates receptor expression, decreasing gonadotropins and gonadal hormone synthesis
Levodopa
Dopamine precursor
converted to dopamine in CNS
Levofloxacin
Respiratory Fluoroquinolone -Ololol gyrating DNA gyrase -oxacins - Flocks of sinners Bactericidal inhibitor of DNA gyrase Other resp fluoro's: gemifloxacin, moxifloxacin
Levonorgestrel
Progestin
used for contraceptives
thickens cervical mucus, inhibits sperm motility, thins endometrium
Lidocaine
Amide local anesthetic
highly selective use-dependent group 1B antiarrhythmic
Little effect on normal cardiac cells, shortens AP duration, no change on ECG (because doesn’t affect normal cells)
nerve block and acute post-MI ischemic ventricular arrhythmia
Lithium
Antimanic
Blocks recycling of the phosphatidylinositol second messenger system
Loratadine
Second gen Antihistamine
H1 blocker, less CNS pen
Losartan
ARB
Angiotensin receptor blocker (AT1 receptor blocker)
Prevents the effects of RAA System, decreases blood pressure
Lovastatin
statin - antihyperlipidemic
HMG-CoA Reductase Inhibitor
Inhibits the rate-limiting step of cholesterol synthesis in hepatocytes, prevents converstion of HMG-CoA to mevalonate, thus decreasing the hepatic pool of cholesterol. In response, the liver upregulates high affinity LDL receptors and clears LDL and VLDL from the blood
[atorvastatin, fluvastatin, pravastatin, rosuvastatin, simvastatin]
Mannitol
Osmotic diuretic
fluid pulled osmotically into the renal tubules
Rx for high ICP and promote excretion of renal toxins in hemolysis/rhabdo
Mebendazole
Antihelminthic
Rx for nematode infection
inhibits microtubule synthesis and glucose uptake in nematodes
[Albendazole, thiabendazole]
Medroxyprogesterone
Progestin (Depo-Provera)
used in combination with an estrogen for menopause or long acting injection
Mefloquine
Antimalarial
Mechanism unknown
Go fuckity fuck yo’ self!
Meperidine
Opioid analgesic
Strong agonist at mu opioid receptors, blocks muscarinic receptors, some serotonergic activity
Equivalent to morphine, but orally available
Metformin
Oral antidiabetic
prototype Biguanide
inhibits hepatic and renal gluconeogenesis through a poorly understood mechanism which involves activation of an AMP-stimulated protein kinase
Methadone
Opioid
synthetic mu agonist, orally available morphine
Methimazole
Antithyroid - small sulfur containing thioamide
blocks peroxidase-catalyzed iodination of the tyrosine residues of thyroglobulin and coupling of DIT and MIT.
Little peripheral inhibition of conversion of T4 to T3
(Propylthiouracil inhibits peripheral conversion)
[Propylthiouracil]
Methotrexate
Antineoplastic, immunosuppressant, DMARD
Cell Cycle-Specific inhibitor of dihydrofolate reductase.
This prevents synthesis of Tetrahydrofolate (THF), which is a necessary intermediary for both protein and purine nucleotide synthesis, interfering with nucleic acid and protein metabolism
Methyldopa
Antihypertensive
prodrug of methylnorepinephrine, a CNS-active alpha2 agonist, reducing SANS outflow from vasomotor center
Metoclopramide
Prokinetic
Dopamine D2 agonist used to stimulate upper GI motility in patients with gastroparesis, also antiemetic
Metronidazole
Antiprotozoal antibiotic
Interferes with nucleic acid synthesis after undergoing a reductive bioactivation of their nitro group by ferrodoxin (present in anaerobic parasites) to form reactive cytotoxic products
[Tinidazole]
Mifepristone
The Stone of Mephistopheles
Medical abortion in early pregnancy, with misoprostol
Progestin and glucocorticoid receptor antagonist
Misoprostol
Prostaglandin E1 derivative, prevents GI ulcers by NSAIDs
abortifacient with mifepristone (the stone of mephistopheles)
Montelukast
Leukotriene receptor blocker (esp. LTD4) used for prophylaxis in asthma
[Zafirlukast]
Morphine
Yum.
Mu opioid receptor agonist.
Nafcillin
Penicillinase-resistant penicillin
Beta-lactam antibiotic, inhibits peptidoglycan cell wall cross-linking
bactericidal
[methicillin, oxacillin, cloxacillin, dicloxacillin]
Naloxone
Opioid mu receptor antagonist
Antidote for opioid overdose
Neostigmine
Cholinesterase inhibitor
synthetic quaternary nitrogen carbamate with little CNS effect
Carbamate binds to Cholinesterase and is immediately hydrolyzed, but the remaining ion portion of neostigmine is slow to dissociate from cholinesterase, thus preventing it from hydrolyzing acetylcholine.
[Pyridostigmine, physostigmine]
Niacin
Vitamin B3
In liver, niacin reduces VLDL synthesis.
In adipose tissue it activates a signaling pathway that reduces hormone-sensitive lipase activity, lowering plasma fatty acid and triglyceride levels.
Reduces catabolism of HDL
Also apparently decreases circulating fibrinogen and increases tpa
Nifedipine
Dihydropyridine Ca Channel Blocker prototype
blocks voltage-gated L-type calcium channels, this decreases intracellular Ca++, reducing muscle contractility and dilating blood vessels
[amlodipine, felodipine, nicardipine]
Nitric Oxide
Endogenous vasodilator released from vascular endothelium
stimulates guanylyl cyclase to make cGMP, which favors dephosphorylation of MLC-PO4 to MLC, which prevents crossbridging and contraction
Nitroglycerin
Antianginal vasodilator
releases NO in veins (less in arteries), causing sm dilation
Decreases preload, which decreases wall tension and thus cardiomyocyte oxygen demand
[isosorbide dinitrate, isosorbide mononitrate]
Norepinephrine
Alpha 1 and 2 agonist, Beta 1 agonist
vasoconstrictor
Olanzapine
Atypical Antipsychotic
High affinity antagonist at 5-HT2a receptorts (as opposed to typical antipsychotics which block D2 receptors)
Blocks positive and negative effects of schizophrenia, few extrapyramidal side effects
[Quetiapine, risperidone, sertindole, clozapine]
Omeprazole
PPI
Irreversible blocker of H/K ATPase propton pump in gastric parietal cells
[Esomeprazole, dexlansoprazole, lansoprazole, pantoprazole, rabeprazole]
Ondansetron
5-HT3 receptor blocker
antiemetic
[Dolasetron, granisetron, palonosetron]
Oseltamivir
Antiviral
Neuraminidase inhibitor
prevents release of mature virions of Influenza A and B
Oxybutynin
Anti Muscarinic
muscarinic cholinoceptor blocker
[Tolterodine]
Paclitaxel
Antineoplastic Plant alkaloid Cell Cycle Specific (M phase) Inhibits mitotic spindle disassembly into tubulin monomers [Docetaxel]
Penicillamine
Chelator,
Bidendate chelator forms two bonds to Copper ion, prevents it from interacting with anything else, easily excreted (water soluble); PCN derivative
Rx: Copper Poisoning/Wilson’s
Penicillin G
IV PCN
Inhibits stage III cell wall synthesis, preventing peptidoglycan cross-linking.
Phenelzine
Irreversible non selective MAOI
Monoamine Oxidase A metabolizes NE & 5HT, MAO B metabolizes Dopamine. Action in Presynaptic axon terminal. Inhibition of metabolism of neurotransmitters leads to increased neurotransmitter storage in vesicles, which results in great amount release into the synaptic cleft.
Phenobarbital
Barbituate
Facilitates GABA-mediated neuronal inhibition by increasing DURATION of channel opening. May block excitatory neurotransmitters
Phenoxybenzamine
Irreversible alpha blocker
Covalently binds to alpha-receptor, non-competitively and irreversibly blocking its activity
[Phentolamine]
Phenytoin
Anticonvulsant
Blocks Na+ channels in neuronal membranes, preventing or slowing depolarization
Tonic-Clonic or Partial Seizures
Pilocarpine
Muscarinic direct acting partial agonist
Increase parasympathetic response
M receptors are Gq (M1, M3, M5) and Gi (M2, M4) which will increase DAG/IP3 and cause sm contraction via Ca++ release, and inhibit Adenylate Cyclase, decreasing cAMP and releasing inhibition MLCK, causing sm contraction
Piperacillin
Extended spectrum PCN with pseudamonas aeruginosa coverage
Pralidoxime
Acetylcholinesterase regenerator
Antidode (with Atropine) for organophosphate poisoning.
Oxime moiety with extremely high affinity for phosphorus in organophosphates, displaces them from the active site of acetylcholinesterase enzyme active site, thus regenerating the enzyme.
Essentially an indirect anticholinergic
Pramipexole
Dopamine D3 agonist in CNS
first line for parkinsonism
[ropinirole, bromocripine (which is more toxic)]
Praziquantel
Antihelminthic
Increases tematode and cestode (fluke and tapeworm) membrane permeability to Ca++, causing muscle contraction followed by paralysis.
[Albendazole, which sounds like a wizard’s name. Albendazole the Aberration Slayer.]
PraZOSIN
Alpha1-selective blocker
for HTN and BPH
[terazosin, doxazosin, Tamsulosin (only for BPH)]
Prednisone
Short acting, potent glucocorticoid
Steroid (S) carried in blood by corticosteroid binding globulin (CBG), S enters cytoplasm and binds receptor which is stabilized by heat-shock protein 90 (HSP90). HSP90 is released, S-Receptor complex forms dimer and enters nucleus to bind glucocorticoid response element (GRE) which alters gene transcription. New mRNA is synthesized, exported to cytoplasm, protein is translated that has ultimate effect.
Probenecid
Uricosuric
Normally 90% of uric acid filtered at kidney is reabsorbed in the proximal tubule, probenecid is a weak acid that competes for reabsorption by the weak acid transport mechanism, thereby increasing uric acid excretion (Low doses it competes with uric acid for secretion into tubule so may actually increase uric acid concentration)
PCNs (and others?) are secreted into the nephron tubule, but this action is inhibited by Probenecid, increasing the half-life. (Presumably via the same general mechanism, a competitive weak acid, that is it competes with PCN for secretion into the tubule)
Procainamide
Group 1A antiarrhythmic
Sodium channel blocker, prolongs the AP duration (see below), slows conduction velocity in atria, purkinje fibers and ventricular cells, some specificity for ischemic tissue but not as much as 1B antiarrhythmics, may abolish abnormal pacemakers if they depend on sodium channels.
Use Dependent
Group 1A’s prolong QT because they have some effect on Potassium current, even though they are considered Sodium Channel blockers. This is why they prolong the AP.
[quinidine]
Propranolol
Non-selective Beta Blocker
Prostacyclin
PGI2, endogenous prostaglandin vasodilator and inhibitor of platelet aggregation (opposite effect of TXA2)
Selective COX-2 inhibitors believed to preferentially inhibit PGI2 over TXA2, leading to thrombotic risks
[epoprostenol, analog used for primary pulm. HTN]
Pyrimethamine
Antiprotozoal
antifolate that inhibits DHF reductase and is synergistic, via sequential blockade, with sulfadiazine against Toxoplasma gondii
Supplement with Folinic acid to offset hematologic tox
Quinine
Antimalarial
Plasmodium undergo primary dev. stage in liver, then parasitize erythrocytes. Quinine is a blood schizonticide, meaning it only affects parasitic forms found in RBCs.
Prevents separation of dsDNA, thus inhibiting genome replication and transcription of mRNA
Ramelteon
Hypnotic
Agonist at brain melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus, for use when onset of sleep is delayed (decreases latency of sleep onset)
Believed to have no abuse potential because no GABA-ergic effect.
Sounds like the name of a Sorcercer. Ramelteon, the Enchanter, will hypnotize you and put you to sleep.
Reserpine
AntiHTN
selective inhibitor of vesicle catecholamine-H+ antiporter (VMAT)
rarely used anymore
Rifampin
Antimicrobial
Part of TB regimen (RIPE, Rifampin, Isoniazid, Pyrazinimide, Ethambutol)
CYP450 Inducer
Inhibitor of DNA-dependent RNA polymerase
[Rifabutin]
Ritonavir
Navir tease a protease Antiviral HIV protease inhibitor (protease cleaves virally encoded proteins to make mature, active virions), often added in low dose combination therapy for AIDS to inhibit metabolism of other drugs CYP450 In'bitor [Indinavir]
Rosiglitazone
Oral antidiabetic
Thiazoldinedione stimulator of peroxisome proliferator-activator gamma nuclear receptors (PPARgamma). Binds nuclear receptor and regulates transcription of genes encoding proteins involved in carbohydrate metabolism. Increases tissue sensitivity to insulin. Increases uptake of glucose in adipose and muscle, inhibits hepatic gluconeo, reduces fasting and postprandial hyperglycemia.
[pioglitazone]
Rivaroxaban
Is a Dragon’s name if I’ve ever heard one.
Rivaroxaban, The Blood Drinker, The Sanguine Scourge, The Tenth Wonder of the World (after King Kong (8th) and the Loch Ness Monster (9th)).
Factor X inhibitor, prevention of DVT, PE, postsurg thromboembolism, and stroke in A. Fib
Selegiline
MAO-B inhibitor
Selectively inhibits MAO-B, which metabolizes Dopamine, thus no tyramine interaction at normal doses. Increases vesicular concentration of Dopamine for greater release after neuronal stimulation. Rx for Parkinson’s.
[Rasagiline]
Sildenafil
PDE-5 inhibitor
Phophodiesterase-5 breaksdown cyclic guanosine monophosphate (cGMP). cGMP dephosphorylates Myosin-LC-PO4 to Myosin-LC, which promotes vasodilation and smooth muscle relaxation.
Inhibition of PDE-5 thus prolongs the effects of cGMP, increasing vasodilation
[Tadalafil, vardenafil]
Sotalol
Group 3 Antiarrhythmic (Potassium Channel Block)
Chiral compound, both isomers block Potassium Channels, and one isomer blocks the beta receptor also.
Slows repolarization, increasing the refractory period and causes visible ECG changes including: Increased PR interval and especially a PROLONGED QT
Spironolactone
K+-Sparring Diuretic
Aldosterone receptor antagonist
Blocks aldo receptor, prevents synthesis and insertion of ENaC into the membrane in Distal Tubule.
Also blocks Androgen receptor, thus Rx for hirsutism.
Eplerenone is more selective aldosterone antagonist, with less anti-androgen receptor effects
Streptogramins
BacteriCIDAL protein synthesis inhibitor antibiotic (most prot. synth. inh.’s are static)
Bind to 50s subunit and constricts exit pore, also decreases tRNA synthetase activity so there is less tRNA in the cell for protein synthesis.
Synercid is a combination of quisupristin and dalfopristin
Used for resistant MRSA, VRE and pneumococcus
[Linezolid, similar use/spectrum, binds 50s, bacterioSTATIC, different class (Oxazolidinone)]
Succinylcholine
Depolarizing neuromuscular relaxant
Nicotinic agonist that depolarizes the NMJ, after initial twitches and fasciculations the muscle relaxes because it is unable to repolarize (necessary for subsequent depolarizations). With continuous infusion, there is a change in the mechanism, it switches from preventing repolarization to increasing resistance to depolarization.
No antidote.
Risk for Malignant Hyperthermia (Rx Dantrolene)
Sulfasalazine
Prodrug metabolized to sulfapyridine and 5-aminosalicylic acid (5-ASA, also known as mesalamine). The sulfapyridine is added to decrease absorption in small intestine, allowing 5-ASA to reach the large intestine where it has topical anti-inflammatory effect, the exact mechanism of which is unknown (perhaps interfering with T Cells or Prostaglandins)
The Sulfapyridine is considered responsible for the systemic adverse effects.
[Mesalamine, balsalazide, olsalazine]
Sumatriptan
5-HT,1d receptor agonist for aborting migraines
5-HT,1d is Gi (decreased cAMP); in the brain it mediates synaptic inhibition via increased potassium conductance
[other -triptans]
Tamoxifen
SERM (selective estrogen receptor modulator)
Rx ER positive breast cancer
Antagonist at breast ER, agonist at endometrial ER, thus carries increased risk of endometrial cancer.
[Toremifene]
[Raloxifene - SERM for osteoporosis, agonist in bone, antagonist at breast and endometrium]
Terbinafine
Antifungal - alters cell membrane permeability
Fungicidal inhibitor of squalene epoxidase, leads to accumulation of squalene, which is toxic because it interferes with ergosterol synthesis. Ergosterol is a sterol specific to fungal cell membranes
most effective for onychomycosis
Tetracycline
Bacteriostatic Antibiotic
Inhibition of protein synthesis. Binds to 30s subunit, prevents incoming binding of charged tRNA to the A site.
[Doxycycline, tigecycline]
Theophylline
Bronchodilator
A naturally occuring methylxanthine found in tea that inhibits PDE. The increased cAMP inhibits myosin-LC kinase, leading to smooth muscle relaxation and bronchiodilation.
[caffeine (coffee), theobromine (cocoa)]
Trimethoprim-sulfamethoxazole (TMP/SMX)
Bactrim
Synergistic sequential blockade of Folate Synthesis. Normally p-Aminobenzoic acid (PABA) is converted to dihydrofolate by dihydropteroate synthase, and DHF is converted to THF by dihydrofolate reductase.
Sulfonamides (like SMX) are structurally similar to and compete with PABA, thus inhibiting the action of dihydropteroate synthase, preventing formation of DHF, and trimethoprim inhibits dihydrofolate reductase, preventing conversion of what DHF is formed to THF.
SMX —-| dihydropteroate synthase (—-| DHF)
TMP —-| dihydrofolate reductase (—-| THF)
Tubocurarine
Non-depolarizing paralytic
competitive nicotinic blocker at NMJ
[pancuronium, atracuronium, vecuronium, other -curiums or -oniums]
Tyramine
Indirect sympathomimetic
releases or displaces NE from stores in nerve endings
Valproic Acid
Anticonvulsant
Treats ALL the seizures, and acts by ALL the mechanisms!
Na+ Channel Blockade: rate-dependent prolongation of inactive state (decreased excitation)
GABA effects: VA inhibits GABA aminotransferase (GABA-T) which terminates the GABA activity (increased inhibition)
Ca++ Channel Blockade: blocks T-type low threshold thalamic Ca++ channels (decreased rhythmic D/C, Rx: abscence seizures)
Other: neuronal membrane hyperpolarization by enhanced K+ channel permeability (both decreased excitation and increased inhibition)
Vancomycin
Bactericidal Antibiotic
Inhibits stage 2 cell wall synthesis by binding D-ala D-ala and preventing polymerization of glycoproteins
Verapamil
L-Type Calcium Channel Blocker
Vasodilator and antiarrhythmic at the AV node
State and use dependent selective depression of calcium channel activity
AV conduction velocity decreased, effective refractory period increased and increased PR interval on ECG
[Diltiazem, nifedipine]
Vincristine
Antineoplastic
Cell Cycle Specific (M Phase)
Inhibits mitotic spindle formation by blocking tubulin dimers from forming microtubules
[vinblastine]
Warfarin
Oral Anticoagulant
Inhibitor of Vitamin K Epoxide Reductase (VKOR), which converts vitamin K epoxide to reduced vitamin K, which is used for postranslational modifaction of clotting factors X, IX, VII, and II
Antidote: Vit K (takes 6-8 hrs), fresh plasma (for acute Rx)
Zidovudine (ZDV)
Antiviral
NRTI, nucleoside reverse transcriptase inhibitor, lacks a 3’ -OH, so when incorporated into DNA synthesis, it causes chain termination
[abacavir, didanosine (ddI), lamivudine (3TC), stavudine (d4T), zalcitabine (ddC)]
Zolpidem
Nonbenzo hypnotic
acts at BZ1 receptor subtype and is reversed by flumazenil
[Zaleplon, eszopiclone]
