Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
69 Cards in this Set
- Front
- Back
|
(m)AChR agonist
- choline ester - restrictively, to diagnose bronchial hyperactivity and asthmatic conditions |
Methacholine
direct CHOLINERGIC AGONISTS |
|
|
AChR agonist
- choline ester - last line drug for wide-angle glaucoma |
Carbachol
direct CHOLINERGIC AGONISTS |
|
|
(m)AChR agonist
-muscarinic - miotic agent, esp. for wide-angle glaucoma (constricts ciliary m and opens Canal of Shlemm) - pilocarpine + physostigmine used for immediate control of intraocular pressure prior to emergency surgery for narrow-angle glaucoma - severe xerostomia following head/neck radiation treatment, other disease states |
Pilocarpine
direct CHOLINERGIC AGONISTS |
|
|
(m)AChR agonist
- choline ester - post-partum and post-operatively (abdominal surgery) to enhance normal fxn. of GI tract and bladder; promotes intestinal motility & tone, urination - decrease esophageal reflux, but not preferred - xerostomia (pilocarpine preferred) |
Bethanechol
direct CHOLINERGIC AGONISTS |
|
|
Competitive AChE antagonist -
rev short acting diagnose myasthenia gravis - brief action |
INdirect:anticholinesterase
short acting Edrophonium |
|
|
Competitive AChE antagonist -
rev - 1st choice for Alzheimer’s - long duration of action, 1x/day |
Donepezil
INdirect:anticholinesterase |
|
|
Competitive AChE antagonist -
rev - 2nd choice for Alzheimer’s - long duration of action, 2x/day |
Rivastigmine
INdirect:anticholinesterase |
|
|
Competitive AChE antagonist -
rev - Alzheimer’s, long duration of action - mild AChE inhibitor & potent allosteric modulator (enhancer) of nAChR - improves cognitive fxn, delays disease |
Galantamine
INdirect:anticholinesterase |
|
|
rev
- 3º amine (crosses BBB) Competitive AChE substrate (slowly hydrolyzed) - topically for wide-angle glaucoma - often w/ pilocarpine for preop narrow-angle glaucoma |
Physostigimine
INdirect:anticholinesterase - 3º amine (crosses BBB) Competitive AChE substrate (slowly hydrolyzed) |
|
|
Competitive AChE substrate (slowly hydrolyzed)
rev poor oral absorption - short duration of action (0.5-2 hr) - drug of choice for paralytic post-op. ileus/atony of GI tract and bladder - drug standard for myasthenia gravis |
INdirect:anticholinesterase
- 4º amine Neostigmine |
|
|
Competitive AChE substrate (slowly hydrolyzed)
rev - same as neostigmine, intermediate duration of action |
Indirect: anticholinesterase
Democurium |
|
|
Competitive AChE substrate (slowly hydrolyzed)
rev - like neostigmine, but longer duration of action (3-6 hr) - drug of choice for myasthenia gravis - prophylaxis for nerve gas |
Indirect: anticholinesterase
Pyridostigmine |
|
|
Organophos-phate
Irrev - glaucoma (the only clinically useful organophosphate) |
Indirect: anticholinesterase
Echothiophate |
|
|
Organophos-phate
Irrev insecticide-paraoxon (pro-drug) |
Indirect: anticholinesterase
Parathion/Malathion |
|
|
Organophos-phate
Irrev nerve gas |
Indirect: anticholinesterase
Sarin/Soman |
|
|
Depolarizing competitive AChR agonist
- phase I blockade: fasiculations - phase II blockade: desensitization - danger of hyperkalemia (can cause cardiac arrest, increased intraocular, intragastric and intracranial pressures) - genetic: bad plasma BuAChE (1/3000) longer duration of action - rare: malignant hyperthermia - bradycardia, esp. in children - not reversed by cholinesterase inhibitor |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Succinylcholine |
|
|
Non-depolarizing competitive nAChR antagonist
Short |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Mivacurium |
|
|
Non-depolarizing competitive nAChR antagonist
Intermediate Liver |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Rocuronium Vecuronium |
|
|
Non-depolarizing competitive nAChR antagonist
Intermediate spontaneous hydrolysis in plasma |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Cisatracurium Atracurium |
|
|
Non-depolarizing competitive nAChR antagonist
Long Kidney deacetylation |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Pancuronium Pipecuronium |
|
|
Non-depolarizing competitive nAChR antagonist
Long Kidney Excretion |
CHOLINERGIC ANTAGONISTS: NEUROMUSCULAR BLOCKERS
Doxacurium Metocurine* Tubocurarine* *Blockade NAcH antagonist |
|
|
Tricyclic amines
- block viral uncoating - oral - excreted unchanged into urine (requires dosage adj. @ renal impairment) Influenza A - works best prophylactically; alleviates symptoms - can treat, vaccinate simultaneously (no suppression of Ab production) Initial therapy for Parkinson’s |
ANTIVIRALS
Amantadine |
|
|
Tricyclic amines
- block viral uncoating - oral - extensively metabolized (no dosage adj.) Influenza A - works best prophylactically; alleviates symptoms - can treat, vaccinate simultaneously (no suppression of Ab production) |
ANTIVIRALS
Rimantadine |
|
|
Neuraminidase inhibitors
- ↓ viral release, ↑ viral aggregation - inhaled as dry powder (poor bioavailability) - 90% excreted unchanged into urine Influenza A and B - works best when administered early - effective prophylactically (not approved) |
ANTIVIRALS
Zanamivir |
|
|
Neuraminidase inhibitors
- ↓ viral release, ↑ viral aggregation - prodrug, well absorbed (80% bioavailability) - excreted unchanged into urine Influenza A and B - works best when administered early - effective prophylactically (not approved) |
ANTIVIRALS
Oseltamivir |
|
|
Nucleoside analogue (guanosine)
1. inhibits viral RNA polymerase (competes w/ GTP, ATP) 2. inhibits GTP synth. (inhibits IMP dehydrogenase ↓ GTP @ infected cell) 3. blocks mRNA capping (inhibits N7 methyl transferase) - water soluble aerosol - oral, not effective Influenza A and B Respiratory syncytial virus Viral hepatitis (w/ interferon) |
ANTIVIRALS
Ribavirin |
|
|
Nucleoside analogues (guanosine)
- acyclovir acyclovir-monophosphate (viral thymidine kinase) acyclovir triphosphate (cellular kinases) 1. inhibits viral DNA polymerase 2. incorporates into DNA, terminates elongation - oral, large doses (insoluble) Neonatal herpes (> acyclovir, but admin. difficult) Herpes encephalitis (1st antiviral agent) |
ANTIVIRALS
Vidarabine |
|
|
Nucleoside analogues (guanosine)
- acyclovir acyclovir-monophosphate (viral thymidine kinase) acyclovir triphosphate (cellular kinases) 1. inhibits viral DNA polymerase 2. incorporates into DNA, terminates elongation - topical Herpes keratitis (drug of choice) |
ANTIVIRALS
Trifluridine |
|
|
Nucleoside analogues (guanosine)
- acyclovir acyclovir-monophosphate (viral thymidine kinase) acyclovir triphosphate (cellular kinases) 1. inhibits viral DNA polymerase 2. incorporates into DNA, terminates elongation - IV, topical (little systemic absorption), oral (15-30% bioavailability) - widely distributed - glomerular filtration, tubular secretion; some metabolism HSV 1 and 2 (@ [low]) Herpes, other strains (@ [high]) Herpes encephalitis (best antiviral) Herpes keratitis Mucocutaneous infections @ immunocomp. pts. (IV) Varicella-zoster @ immunocomp. pts. |
ANTIVIRALS
Acyclovir (Acycloguanosine) |
|
|
Nucleoside analogues (guanosine)
- acyclovir acyclovir-monophosphate (viral thymidine kinase) acyclovir triphosphate (cellular kinases) 1. inhibits viral DNA polymerase 2. incorporates into DNA, terminates elongation - IV @ acute - oral @ maintenance Cytomegalovirus retinitis (serious infections only) Pneumonia due to CMV @ kidney transplant pts. (w/ anti-CMV Ab) |
ANTIVIRALS
Ganciclovir |
|
|
Nucleoside analogue (cytosine)
- IV CMV retinitis @ ganciclovir resistance |
ANTIVIRALS
Cidofovir |
|
|
Pyrophosphate analogue
- interact w/ PPi binding site inhibit DNA polymerase, reverse transcriptase - IV CMV retinitis @ ganciclovir resistance, pt. intolerance (but more expensive, less well tolerated) |
ANTIVIRALS
Focarnet |
|
|
Glycoproteins
Activates cellular expression: 1. kinase inhibits replication (inactivates IF) 2. endonuclease degrades viral mRNA 3. phosphodiesterase degrades tRNA inhibits peptide elongation - IM - subQ - topical Chronic Hepatitis B and C (w/ ribavirin, synergistic, side effects min. criteria for Tx) [> interferon alone] Hairy cell leukemia AIDS-related Kaposi’s sarcoma Genital warts condyloma acuminatum Herpes zoster (if given early can prevent viral dissemination @ cancer pts.) Herpes Keratoconjunctivitis (w/ other antivirals) |
ANTIVIRALS
Interferons |
|
|
A Antagonist Non-selective
A1 & A2 Reversible - blocks vasoconstriction, decreases TPR and BP, causes reflex tachycardia - blocks cardiac alpha2, increase E and NE release from chromaffin cells in myocardium (tachycardia, ↑CO) - IV - short duration (1-2hr) - pre-op. for pheochromocytoma (avoid hypertensive crisis) - can be used instead of dopamine in cases of shock (blocks reflex vasoconstriction, maintains tissue perfusion) |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Phentolamine |
|
|
Antagonist Non-selective
A1 & A2 Irreversible - blocks vasoconstriction, decreases TPR and BP, causes reflex tachycardia - blocks cardiac alpha2, increase E and NE release from chromaffin cells in myocardium (tachycardia, ↑CO) - IV or PO - long duration (12-24 hr) - pheochromocytoma: pre-op (avoid hypertensive crisis) and long-term for malignant/inoperable cases - Raynaud’s, other peripheral vascular diseases |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Phenoxybenzamine |
|
|
Antagonist
Selective A1 - blocks vasoconstriction, decreases TPR and BP, no reflex tachycardia, no change in CO - PO - long duration (12-24 hr) [longest: Doxazosin] - metabolized in liver - anti-hypertension - benign prostatic hypertrophy |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Prazosin - prototype Terazosin Doxazosin - #1 Tamsulosin - new |
|
|
Adrenergic Neuronal Blockers
- competes with tyr for tyrosine hydroxylase, instead of tyr à dopa à DA à NE, met-tyr à met-NE (a false neurotransmitter) - not used clinically |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Metyrosine |
|
|
Adrenergic Neuronal Blockers
- blocks packaging of NE into vesicles by inhibiting Mg-dependent Na-K ATPase - decreases sympathetic fxn (decreased BP and bradycardia) - PO, IM, IV - delayed onset (gradual depletion of NE), long duration of action - anti-hypertension |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Reserpine |
|
|
Adrenergic Neuronal Blockers
- hydrolyzes NE-ATP in vesicles - IV - delayed onset - emergency hypertension |
ADRENERGIC ANTAGONISTS: a, NEURONAL BLOCKERS
Guanethidine Guanadrel |
|
|
very poor
- IV - topical - oral: GI fungi (topical) - broadest spectrum antifungal - drug of choice for life-threatening systemic infections - invasive Aspergillus (w/ itraconazole) - cryptococcal meningitis (w/ flucytosine), [alternative: fluconazole] - histoplasmosis - dermatophytic, mucocutaneous infections |
ANTIFUNGALS
Amphotericin B - polyene macrolide - binds sterols in plasma membrane (esp. ergosterol), forming cytotoxic pores |
|
|
extremely poor - topical only (incl. GI) due to toxicity - local (dermal), oropharyngeal infections
- vaginal candidiasis |
ANTIFUNGALS
Nystatin - polyene macrolide - binds sterols in plasma membrane (esp. ergosterol), forming cytotoxic pores |
|
|
good - oral only
- only in combinations (but resistance, toxicity) - cryptococcal meningitis (w/ amphotericin B) - blastomycoses (w/ itraconazole) |
ANTIFUNGALS
Flucytosine - antimetabolite - converted by fungi to active metabolites - inhibits fungal RNA/DNA synthesis |
|
|
poor
- ↑ w/ fatty foods - oral (micro-crystalline form) - dermatophytosis (esp. nail infections [terbinafine preferred]) requiring extended Tx (after or w/ triazoles) - athlete’s foot, ringworm |
ANTIFUNGALS
Griseofulvin - cytoskeleton agent - inhibits microtubules blocks fungal mitosis (fungistatic) - binds keratin |
|
|
low
- ↑ w/ food, low gastric pH - ↓ w/ rifampin, H2 antagonists, antacids - oral (slow onset) - mucocutaneous candidiasis - coccidioidomycosis (non-meningeal) - seborrheic dermatitis (in shampoos) [largely supplanted by itraconazole/fluconazole] |
ANTIFUNGALS
Ketoconazole - imidazole - inhibits fungal ergosterol synthesis - selectively inhibits fungal P450 enzymes |
|
|
extremely poor - topical
(clotrimazole - oral troches) - topical antifungals (OTC, common) - vulvovaginal candidiasis - dermatophytic infections - oropharyngeal thrush (candidiasis; alt. to nystatin) |
ANTIFUNGALS
Miconazole Clotrimazole - imidazole - inhibits fungal ergosterol synthesis - selectively inhibits fungal P450 enzymes |
|
|
OK, low bioavailability (no CSF)
- ↑ w/ food, low gastric pH - oral - most potent of azoles for systemic infections - drug of choice for persistent dermatophytosis - only agent effective for all Aspergillus infections - preferred for endemic mycosis (e.g. Histoplasma) |
ANTIFUNGALS
Itraconazole - triazole - inhibits fungal ergosterol synthesis |
|
|
good (excellent CSF) - oral
- IV - drug of choice for cryptococcal meningitis (unless life-threatening amphotericin B) - mucocutaneous candidiasis - prophylactic @ bone marrow transplants, AIDS pts. |
ANTIFUNGALS
Fluconazole - triazole - inhibits fungal ergosterol synthesis |
|
|
- topical
- oral (terbinafine) - most cutaneous mycoses (topical) - nail infections (oral terbinafine) - not effective against Candida |
ANTIFUNGALS
Naftifine Terbinafine - allylamine - inhibits fungal squalene metabolism (↑ squalene toxic), ↓ ergosterol |
|
|
poor (highly protein-bound) - IV (once daily) - invasive candidiasis
- aspergillosis (alt. to amphotericin B) - not effective against cryptococcus |
ANTIFUNGALS
Caspofungin - echinocandin - inhibits β (1,3)-D-glucan (cell wall) synthesis |
|
|
Acebutolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
S PO |
|
|
Atenolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
S - #1 for HTN PO - no CNS effects lowest lipid solubility |
|
|
Esmolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
S IV - anti-arrhythmic (despite lack of MSA) |
|
|
Metoprolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
S PO highest lipid solubility |
|
|
Naldolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS PO |
|
|
Pindolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS PO - ISA: good for CHF |
|
|
Propranolol
- prototype |
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS highest lipid solubility PO/IV - anti-arrhythmic - MSA: mouth gets numb |
|
|
Timolol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS PO - #1 for glaucoma for chronic Tx (decreases aqueous humor production, 2) [for acute Tx, use pilocarpine |
|
|
Sotalol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS PO - anti-arrhythmic (atrial fibrillation) - no longer used for HTN, angina, hyperthyroidism |
|
|
Labetalol
|
ADRENERGIC ANTAGONISTS: β BLOCKERS
NS - #1 for HTN in ER PO - does NOT cause cold fingers (an A effect) |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - reverse muscarinic or anti-AChE poisoning - to producelong-lasting mydriasis and cycloplegia - with diphenoxylate (mild opioid agonist), an effective anti-diarrheal |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Atropine - 3º amine (crosses BBB) |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - motion sickness |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Scopolamine - 3º amine (crosses BBB) |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - bronchodilator (esp. for COPD) |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Ipratropium - 4º amine |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - non-obstructive irritable bowel syndrome, other GI disturbances - ulcers (not preferred) - excessive sweating |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Propantheline - 4º amine |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - overactive bladder (w/ increased urinary frequency or urgency, incontinence) |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Oxybutynin Tolterodine |
|
|
Anti-muscarinic
(competitive mAChR antagonist) - short-acting mydriatic agent |
CHOLINERGIC ANTAGONISTS: ANTI-MUSCARINICS AND GANGLIONIC BLOCKERS
Tropicamide |
|
|
Depolarizing
(competitive nAChR agonists) - smoking cessation - stimulation of autonomic ganglia (followed by ganglionic blockade), adrenal medulla (catecholamine secretion), CNS (alerting response/change in respiration) |
Ganglionic blocker
Nicotine |
|
|
Non-depolarizing
(competitive autonomic ganglia nAChR antagonists) - improve GI absorption (decreases GI motility) - used in Tourette’s syndrome |
Ganglionic blocker
Mecamylamine - 3º amine (crosses BBB) |
|
|
Non-depolarizing
(competitive autonomic ganglia nAChR antagonists) - research only - 1st effective anti-hypertensive |
Ganglionic blocker
Hexamethonium (C6) |
|
|
Non-depolarizing
(competitive autonomic ganglia nAChR antagonists) - research only |
Ganglionic blocker
Tetraethylammonium |
