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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