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209 Cards in this Set
- Front
- Back
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Bethanecol
(MOA) |
Muscarinic agonist w/ selective GI & GU effects
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Bethanecol
(Pharm Effects) |
Increase acid secretion, motility & tone, relax sphincters, stim secretion in GI tract, contract detrusor muscle & relax ext sphincter
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Bethanecol
(Therapeutic Uses) |
*bowel stasis
*post op paralytic ileus *urinary retention (post op or neurological) |
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Bethanecol
(Adverse Effects) |
Contraindications:
*asthma *COPD *peptic ulcer *CHF *hyperthryroidism |
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Succinylcholine
(MOA) |
Exhibits specificity for N2 cholinergic receptors in NMJs of sk muscle.
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Succinylcholine
(Pharm Effects) |
1. NM blocking drug
- IV bolus causes initial contraction followed by a flaccid paralysis lasting 3-5 min. - Plasma cholinesterase determines quantity of drug to reach NMJ - Termination of action is determined by diffusion |
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Pilocarpine
(MOA) |
- Muscarinic receptor agonist
- Not metabolized by AChase or pseudocholinesterase |
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Pilocarpine
(Pharm Effects) |
Contraction of meridional fibers of ciliary muscles > Increases iridiocorneal angle > Increasing outflow of aqueous humor
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Pilocarpine
(Therapeutic Uses) |
Glaucoma
Dry Mouth (Sjogren's syndrome) |
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Pilocarpine
(Adverse Reactions) |
In trmt of glaucoma:
*lens fixation impairs far vision *persistent miosis causes poor night vision Contraindications: *asthma & COPD (bronchoconstriction) *peptic ulcer (increased production of gastric acid) *hyperthyroidism (atrial flutter or fib) *dilated heart (atrial flutter or fib) |
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Betaxolol
(MOA) |
Beta-adrenoreceptor antagonist
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Betaxolol
(Pharm Effects) |
- Decreases aqueous humor
- Decreases IOP 20-30% |
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Betaxolol
(Therapeutic Uses) |
Open Angle Glaucoma
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Betaxolol
(Adverse Reactions) |
Systemic absorb-bradycardia
(Selective for B1-little effect on bronch smooth muscle) |
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Timolol
(MOA) |
Beta-adrenoreceptor antagonist
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Timolol
(Pharm Effects) |
Decrease production of aqueous humor
Lower IOP by 20-30% |
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Timolol
(Therapeutic Uses) |
Glaucoma
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Timolol
(Adverse reactions) |
Systemic absorption can cause bronchoconstriction & bradycardia
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Lantanoprost
(MOA) |
Stable analog of PGF 2alpha
(prsostaglandin analog) |
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Lantanoprost
(Pharm Effects) |
-Increase uveoscleral outflow
(Only drug that enhances this) - Lower IOP by 20-25% |
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Lantanoprost
(Therapeutic Uses) |
Open Angle Glaucoma
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Epinephrine
(MOA) |
Alpha1-adrenoreceptor agonist
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Epinephrine
(Pharm Effects) |
-Enhance outflow of aqueous humor via nl press dep path.
-Decreases IOP |
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Epinephrine
(Therapeutic Uses) |
Open Angle Glaucoma
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Epinephrine
(Adverse Reactions) |
Causes mydriasis via stimulation of alpha1 adrenoreceptors in the radial muscle of the iris
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Dipivefrin
(MOA) |
Alpha-adrenoreceptor agonist
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Dipivefrin
(Pharm Effects) |
-Lipid soluble cmpd that penetrates into the ant chamber before being hydrolyzed to epinephrine
-enhance outflow of aqueous humor via nl press dep path |
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Dipivefrin
(Therapeutic Uses) |
Open Angle Glaucoma
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Dipivefrin
(Adverse Reactions) |
Causes mydriasis via stimulation of alpha1 adrenoreceptors in the radial muscle of the iris
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Dorzolamide
(MOA) |
Carbonic anhydrase inhibitor
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Dorzolamide
(Pharm Effects) |
-Topical decrease production of aqueous humor
-Decrease IOP by 10-20% |
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Dorzolamide
(Therapeutic Uses) |
Glaucoma
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Donepezil
(MOA) |
Carbamate cmpd that is a Reversible inhibitor of AChase
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Donepezil
(Pharm Effects) |
Inhibits the action of acetyl cholinesterase so that acetylcholine will stay around longer
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Donepezil
(Therapeutic Uses) |
DOC for Alzheimer’s dz- it is more selective for the CNS
Decreases apathy, hallucinations, anxiety & behavioral problems |
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Donepezil
(Adverse Reactions) |
S/E:
Diarrhea Muscle cramps Fatigue Insomnia Anorexia N/V |
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Neostigmine Quarternary
(MOA) |
4º amine
Direct agonist at cholinergic N2 receptor, inhibits AChase (by carbamoylation) at all peripheral sites |
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Neostigmine Quarternary
(Pharm Effects) |
Increases the conc of acetylcholine at N2 receptor of NMJ by blocking AChase, inhibition of AChase increases the conc of ACh at muscarinic sites (eg heart, salivary glands, etc)
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Neostigmine Quarternary
(Therapeutic Uses) |
*post op paralytic ileus
*atony of the GI & GU tracts *Myasthenia gravis *reversal of the muscle paralysis caused by competitive neuromuscular blocking agents |
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Pyridostigmine
(MOA) |
4º amine
Direct agonist at cholinergic N2 receptor, inhibits AChase (by carbamoylation) at all peripheral sites. |
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Pyridostigmine
(Pharm Effects) |
Inhibits the action of acetyl cholinesterase so that acetylcholine will stay around longer
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Pyridostigmine
(Therapeutic Uses) |
Long-term p.o. dosing used to treat Myasthenia gravis:
*mild ocular symptoms- pyridostigmine + corticosteroids *mild/mod general symptoms- pyridostigmine + thymectomy *mod/severe general symptoms- pyridostigmine + azathioprine (an immunosuppressant drug) |
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Edrophonium
(MOA) |
Even though it does inhibit AChase at all peripheral cholinergic nerve junc (carbamoylation of active site), the majority of its action at the NMJ results from direct stim of cholinergic N2 receptors
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Edrophonium
(Pharm Effects) |
*must be given im or iv b/c of extremely short half life
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Edrophonium
(Thearpeutic Uses) |
diagnosis of & titrate adequacy of trmt of myasthenia gravis
*distinguish between “myasthenic” & “cholinergic” crisis in pts treated p.o. w/ pyridostigmine *reversal of muscle paralysis caused by competitive neuromuscular blocking agents such as d-tubocurarine |
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Carbaryl
(MOA) |
Carbamate (insecticide used around the house).
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Carbaryl
(Thearapeutic Uses) |
Treat carbaryl poisoning w/ atropine (only drug) & supportive care
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Carbaryl
(Adverse Reactions) |
CNS-Loss of concentration, irritability, forgetfulness, depression, insomnia, slurred speech.
PNS-Miosis, blurred vision, bradycardia, cough Nicotinic-Cramping, tachycardia |
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Malathion [Insecticide]
(MOA) |
Insecticide that is much safer than parathion, mammals & birds have plasma carboxyesterases which destroy malathion
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Malathion [Insecticide]
(Therapeutic Uses) |
Spray for mosquitos and in dermatological preparations used to kill head lice
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Pralidoxime
(MOA) |
-Accelerates the rate of hydrolysis of phosphorylated enzyme, at NMJ.
-Less effective if aging of phosphorylation has occurred |
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Pralidoxime
(Therapeutic Uses) |
Treatment for organophosphate poisoning with Atropine!
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DOC for relieving priaprism
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Epi (adrenalin) mixed alpha,beta
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DOC for mydriasis
Fundoscopic exam |
tropicamide
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DOC for
uveitis, keratitis, choroiditis |
atropine or scopolamine
relaxation of sphincter |
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DOC for HTN in pregnant woman
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alpha methyldopa
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DOC for alzheimers disease
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donepezil
aricept |
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DOC for treatment of anaphylactic reactions
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epinephrine
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cholinergic agonist
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succinylcholine
bethanechol pilocarpine |
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tertiary muscarinic blockers
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diphenhydramine
cyclopenate - receptor scopolamine - receptor tropicamide atropine benzotropine |
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carbonic anhydrase inhibitor
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dorzolamide
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treatment for organophosphate poisoning
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pralidoxime
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quartenary muscarinic blocker
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ipratropiam
glycopyriolate |
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adrenergic agonist
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ephederine
citrodrine oxymetazoline albuterol epi-alpha isoproterenol nor-epi dopamine phenylephrine dipivefrin |
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tertiary carbmate achase inhibitor
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carbaryl
dicylamine donepezil |
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tertiary muscarinic agonist
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tolterodine
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alpha blockers
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labetalol
tamsulosin phentolamine |
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beta blockers
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betaxolol
propanolol esmolol metoprolol atenolol timolol |
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tertiary amines
vs quartenary amines |
tertiary: Enter CNS-Placenta, eye, breast milk, semen
Quartenary: do not |
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Quartenary carbamate achase inhibitor
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pyridostigmine
neostigmine edrophonium |
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sympathetic drug
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alpha-methyldopa
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why dobutamine over dopamine in tx of MI
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dobutamine does not increase DBP (afterload)
dobutamine is less likely to cause tachycardia dobutamine causes venodilation which decreases venous return (preload), so cardiac filling pressure is decreased. |
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Pralidoxime
MOA |
Quaternary:
Greatly accel the rate of hydrolysis of the phosphorylated enzyme, particularly at NMJ, less effective if “aging” of phosphorylation has occurred, does not enter CNS |
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Atropine
MOA |
1. muscarinic receptor antagonist (Belladonna alkaloids)
2. Tertiary amines enter CNS, cross plancental barrier, penetrate into eye, and pass into breast milk and semen. 3. Blocks central/peripheral muscarinic receptors |
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Atropine
Pharm Effects |
Muscarinic antagonists:
Iris: sphincter relaxation (no miosis) Ciliary relaxation (no near vision) Cardiac: ↑ atrial & ventricle contraction ♥ conduction: ↑ HR, atrial conduction velocity, AV conduction velocity and automaticity, ↓ APD/ERP Bronchi relaxation GI tract ↓ motility and tone GU detrusor relaxes & sphincter contract ↓ secretion of saliva, lacrimal, sweat, gastric juice, bronchial |
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Atropine
Therapuetic Uses |
1. Treats organophosphate poison
2. Treats carbamate poisoning along with pralidoxime 3. Perioperative use: -Used to decrease production of saliva/pulmonary secretions -Counteracts the bradycardia caused by ocular pressure, visceral traction, carotid sinus stimulation or injection of multiple doses of succinylcholine -reverse competitive neuromuscular blockade caused by drugs like d-turbocurarine -prevents unwanted muscarinic stimulation which result in the inhibition of AChase at sites innervated by the PNS 4. Ophthalmology: -Use for determination of refractive error -DOC for Tx of anterior uveitis, keratitis , & choroiditis; Relaxation of sphincter & ciliary muscles decrease pain -Used in cataract surgery which req mydriasis for access to lens sac via the pupil 5. CV disease: -Reversal of digoxin induced AVB -Reversal of bradycardia in kids -Tx of hyperactive carotid sinus syndrome 6. GI disease -Diphenoxylate+atropine (Limotil) for diarrhea: very small atropine dose req to prevent abuse of diphenoxylate opiate (↓ GI motility) 7.Prevents indirect adverse S/E’s of neostigmine & pyridostigmine 8. Blocks central muscarinic receptors: (Parkinson’s Ds) |
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Atropine
Adverse Effects |
1. Parkinson’s Ds.: Cycloplegia, constipation, urinary retention, and dry mouth
Toxicity of atropine-like drugs: CNS: nervousness, excitation, confusion, hallucinations, weakness, giddiness, muscular incoordination, hypertension, maniacal tendencies. PNS: dry mouth, thirst, dysphagia, hot/dry/flushed skin, dilated pupils, photophobia, blurred vision, tachycardia, urinary retention, absence of bowel sounds. Overdose: red as a beet (cutaneous dilation), hot as pistol (hot skin), mad as a hatter (hallucinations/delirium), and dry as a desert (inhibition of salivation/difficulty swallowing) |
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Scopolamine
MOA |
Muscarinic antagonist (Belladonna alkaloids
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Scopolamine
Pharm Effects |
Relaxes ciliary (no near vision) &/or sphincter muscle (no miosis
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Scopolamine
Therapeutic Uses |
1. Ophthalmology:
-Used in determination of refractive error -DOC: Tx of anterior uveitis, keratitis, & choroiditis; Relaxation of sphincter & ciliary muscles dec pain -Used in cataract surgery which req mydriasis for access to lens sac via the pupil. 2. Motion sickness (prophylactically) |
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Scopolamine
Adverse Effects |
Therapeutic doses can cause somnolence, euphoria, amnesia, and dreamless sleep (reduced REM sleep); Little effect on heart rate.
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Cyclopentolate
MOA |
Muscarinic antagonist
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Cyclopentolate
Pharm Effects |
Relaxes ciliary (no near vision) &/or sphincter muscle (no miosis)
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Cyclopentolate
Therapeutic Uses |
Ophthalmology:
-Used in determination of refractive error -Used in cataract surgery which req mydriasis for access to lens sac via the pupil. |
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Tropicamide
MOA |
Muscarinic antagonist
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Tropicamide
Pharm Effects |
1. Mydriasis
2. Short duration of action 3. Cannot penetrate into the ciliary muscle |
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Tropicamide
Therapeutic effects |
Opthalmology:
-DOC for fundoscopic exam requiring mydriasis in thorough exam of retina & optic disc |
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Benztropine
MOA |
Central muscarinic antagonist
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Benztropine
Therapeutic Uses |
Parkinson’s dz: most effective in tremor, some effect on rigidity, little effect on akinesia/ dyskinesia
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Benztropine
Adverse Reaction |
Cycloplegia, constipation, urinary retention, and dry mouth (therefore, limited in Parkinson’s dz).
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Dicyclomine
MOA |
Muscarinic antagonist
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Dicyclomine
Therapeutic Uses |
GI dz: prevent bowel spasm & dec the pain associated with irritable bowel syndrome
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Tolterodine
MOA |
Selective M3-muscarinic receptor antagonist effective in tx of urge intcontinence
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Tolterodine
Therapeutic Effects |
OAB/Urinary incontinence
Prevent post-prostatectomy bladder spasms |
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Tolterodine
Adverse Reaction |
Somnolence, dry mouth, blurred vision, constipation
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Solifenacin
MOA |
Selective M3-muscarinic receptor antagonist
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Solifenacin
Pharm Effects |
Fewer CNS effects
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Solifenacin
Therapeutic Uses |
DOC for OAB/urinary incontinence
Prevent post-prostatectomy bladder |
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Solifenacin
Adverse Reaction |
Less dry mouth
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Darifenacin
MOA |
Selective M3-muscarinic receptor antagonist
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Darifenacin
Pharm Effects |
No CNS or CV effects
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Darifenacin
Therapeutic Uses |
DOC for OAB/urinary incontinence
Prevent post-prostatectomy bladder spasms |
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Darifenacin
Adverse Reaction |
Less dry mouth
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Diphenhydramine
(benadryl) MOA |
Muscarinic antagonist
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Diphenhydramine
(benadryl) Pharm Effects |
Antihistamine that blocks central muscarinic receceptor
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Diphenhydramine
(benadryl) Therapeutic Uses |
Parkinson’s dz: most effective in tremor, some effect on rigidity, little effect on akinesia/ dyskinesia
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Diphenhydramine
(benadryl) Adverse Reaction |
Cycloplegia, constipation, urinary retention, and dry mouth (therefore, limited in Parkinson’s dz)
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Ipratropium
MOA |
Muscarinic antagonist
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Ipratropium
Pharm Effects |
Relaxes bronchial smooth muscle
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Ipratropium
Therapeutic Effects |
COPD (bronchitis+emphysema) Imporves ventilation by relaxing bronchial smooth muscle
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Glycopyrrolate
MOA |
Muscarinic antagonist
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Glycopyrrolate
Therapeutic Uses |
Perioperative use:
-Used to decrease production of saliva/pulmonary secretions -Counteracts the bradycardia caused by ocular pressure, visceral traction, carotid sinus stimulation or injection of multiple doses of succinylcholine -Prevents unwanted muscarinic stimulation which result in the inh of AChase at sites innervated by the PNS. |
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Varenicline
MOA |
1. Partial agonist at central α4 β2 – nicotinic receptors
2. 50% of the intrinsic activity of nicotine |
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Varenicline
Pharm Effects |
1. causes the release of dopamine from the nucleus accumbens
2. blocks the binding of nicotine to α4 β2 – nicotinic receptors |
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Varenicline
Therapeutic Effects |
Smoking cessation
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Varenicline
Adverse Reaction |
Nausea, insomnia, headache, abnormal dreams, constipation, abdominal pain
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Dopamine
MOA |
D1>β1>α1
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Dopamine
Pharm Effects |
Know the doses
Low i.v. dose: 0.5-2.0 μg/kg/min stimulates D1 dopamine receptors = dilates renal afferent arterioles Intermediate iv dose: 2-10 μg/kg/min stimulates D1 and B1 receptors = ↑ dp/dt Large dose: >10 μg/kg/min stimulate a-receptors in resistance arterioles = ↑ TPR & DBP/afterload |
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Dopamine
Therapeutic Effects |
Used to increase BP in hemorrhagic & septic shock and increase CO after MI
Used to increase CO in CHF which is refractory to digoxin plus diuretic drugs Used to increase urine flow in the tx of barbiturate and salicylate poisoning (inc in RBF results from inc CO and direct renal vasodilation). Small doses used to maintain urine flow in ICU. |
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Dopamine
Adverse Reaction |
1. Cerebrovascular hemorrhage
2. Pulmonary edema 3. B-agonist action: cardiac arrhythmias, angina in CAD patients 4. a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of a-adrenoceptor agonist |
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Dobutamine
MOA |
B1≥B2
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Dobutamine
Pharm Effects |
1. (+) inotropic effects via B1 stimulation ↑SV
2. Arteriolar dilation via B2 stimulation lowers TPR so DBP may fall slightly. 3. Venodilation via B2 stimulation decreases venous return & thus decreases venous filling pressure in pts with MI. 4. Unlike dopamine, dobutamine has little effect on HR at most clinical doses. Excessive doses can cause tachycardia & cardiac dysrhythmias. 5. increase in GFR results solely form the increase in CI, i.e., no effect at renal D1 receptors. |
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Dobutamine
Therapeutic Uses |
Used to increase CO after MI, septic, and Cardiogenic shock
Advantages over dopamine in MI tx: 1. does not inc DBP 2. less likely to cause tachycardia 3. causes venodilation which dec venous return (preload), so cardiac filling pressure is decreased. |
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Dobutamine
Adverse Reaction |
1. Tremor with B2 action
2. B-agonist action: cardiac arrhythmias, angina in CAD patients |
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Norepinephrine
MOA |
α>β1>β2
Pure α-receptor stimulation |
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Norepinephrine
Pharm Effects |
-Direct CV effects: ↑ TPR, DBP
-Indirect CV effects: bradycardia |
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Norepinephrine
Therapeutic Effects |
Used as vasopressor agent when CO & tissue perfusion are relatively normal (spinal shock)
Vasoconstrictor agent with local anesthetic drugs |
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Norepinephrine
Adverse Reaction |
B-agonist action: cardiac arrhythmias, angina in CAD patients
a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of a-adrenoceptor agonist esp NE Cerebrovascular hemorrhage Pulmonary edema |
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Epinephrine
(adrenalin) MOA |
β2>β1>α
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Epinephrine
(adrenalin) Therapeutic Effects |
1. Bronchodilator in patients with asthma & COPD
2. Local application lowers intraocular pressure by increasing outflow of aqueous humor (a1) 3. Vasoconstrictor agent with local anesthetic drugs 4. DOC for the tx of anaphylactic reactions (reverses bronchodilation and laryngeal edema) 4. DOC for relieving priapism (persistent painful erection) 5. Uses as a positive inotropic & chronotropic agent in cardiac arrest (1/3 saved) |
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Epinephrine
(adrenalin) Adverse Reactions |
Anxiety
B-agonist action: cardiac arrhythmias, angina in CAD patients a-agonist: renal and mesenteric ischemia Cerebrovascular hemorrhage Pulm edema from prolonged TPR increases. Tremor with B2 action |
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Isoprotenerol
MOA |
B1=B2
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Isoprotenerol
Therapeutic Effects |
Increases AV conduction in AV block.
Used as a positive inotropic & chronotropic agent in cardiac arrest. |
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Isoprotenerol
Adverse Reactions |
B-agonist action: cardiac arrhythmias, angina in CAD patients
Cerebrovascular hemorrhage Tremor with B2 action |
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Albuterol
MOA |
B2>>B1
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Albuterol
Therapeutic Effects |
Used to relieve the bronchoconstriction associated w/ asthma, COPD, & bronchitis with less tachycardia
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Albuterol
Adverse Reactions |
B-agonist action: cardiac arrhythmias, angina in CAD patients
Tremor with B2 action |
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Ritodrine
MOA |
B2>>B1
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Ritodrine
Therapeutic Uses |
1. Used to relax uterine smooth muscle in order to delay parturition.
2. Used to relax uterine smooth muscle in order to achieve external version of a fetus from breech position to a vetex position prior to birth. 3. Used to relieve the bronchoconstriction associated w/ asthma, COPD, & bronchitis with less tachycardia |
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Ritodrine
Adverse Reaction |
B-agonist action: cardiac arrhythmias, angina in CAD patients
Tremor with B2 action |
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Phenylephrine
MOA |
α1 only
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Phenylephrine
Therapeutic Uses |
Systemic vasoconstrictor agent (increase B/P)
Local application: 1. relieves nasal congestion by constricting the blood vessels of the nasal mucosa. 2. produces mydriasis by contraction of the radial muscle of the iris / Used for fundoscopic exams and ocular surgery |
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Phenylephrine
Adverse Reaction |
a-agonist: renal and mesenteric ischemia
Cerebrovascular hemorrhage |
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Oxymetazoline
(Afrin) MOA |
α only
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Oxymetazoline
(Afrin) Therapeutic Uses |
Used as a nasal decongestant.
Longer duration of action than phenylephrine |
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Oxymetazoline
(Afrin) Adverse Reaction |
a-agonist: renal and mesenteric ischemia
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d-amphetamine
MOA |
Indirect acting agonist
no direct agonist effect at adrenoreceptor |
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d-amphetamine
Pharm Effects |
1. Cause the release of endogenous NE stored in noradrenergic fibers.
2. Inc B/P to some extent b/c they release NE from the sympathetic nerves which innervate the blood vessels |
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d-amphetamine
Therapeutic Effects |
Used to treat ADHD and ADD
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d-amphetamine
Adverse Reaction |
Insomnia
Psychiatric disturbance a-agonist: renal and mesenteric ischemia / mesenteric arterioles rapidly “escape” from the vasoconstrictor effects of a-adrenoceptor agonist esp NE Cerebrovascular hemorrhage |
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Ephedrine
MOA |
Mixed agonist
1. Direct B1 & B2 adrenoreceptor 2. indirect: releases endogeous NE which acts at a- & B-adrenoceptors |
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Ephedrine
Pharm Effects |
Direct B-adrenoceptor mediated actions cause bronchodilation in asthma & increased HR, CO, &, AV conduction in AV block.
Indirect a-adrenoceptor mediated actions produce mydriasis, increased B/P, and nasal decongestion. -Central excitation d/t release of NE in the brain (milder than amphetamine -Lipid soluble: enters CNS |
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Ephedrine
Therapeutic Uses |
Used as nasal decongestant
Used as a pressor agent to reverse hypotension during anesthesia |
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Ephedrine
Adverse Reaction |
Insomnia
B-agonist action: cardiac arrhythmias, angina in CAD patients a-agonist: renal and mesenteric ischemia Cerebrovascular hemorrhage Tremor with B2 action. Rebound nasal congestion |
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Pseudoephedrine
(Sudafed) MOA |
Mixed agonist
Stereoisomer of ephedrine Lipid Soluble: enters CNS |
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Pseudoephedrine
(Sudafed) Pharm Effects |
Causes less CNS excitation and less of an increased BP & HR as compared to ephedrine
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Pseudoephedrine
(Sudafed) Therapeutic Uses |
Used as nasal and sinus decongestant
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Pseudoephedrine
(Sudafed) Adverse Reactions |
Insomnia
B-agonist action: cardiac arrhythmias, angina in CAD patients a-agonist: renal and mesenteric ischemia Cerebrovascular hemorrhage Tremor with B2 action. Rebound nasal congestion |
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Tamsulosin
MOA |
a-antagonist
a-blockers selective for α1a: abundant in smooth muscle of prostate, prostatic capsule, prostatic urethra, and bladder neck / 70% of receptors are a1A-subtype |
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Tamsulosin
Therapeutic Uses |
Prostatic hypertrophy: relieve urinary obstruction to increase urine flow rate
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Tamsulosin
Adverse Reaction |
Same as phentolamine, except for angina
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Phentolamine
MOA |
a-antagonist
a-blockers (α1=α2) |
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Phentolamine
Pharm Effects |
CV effects in HTN w/ normal cardiac fxn: ↓ TPR & BP, ↑ HR, dp/dt, & venous capacitance; no effect on CO
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Phentolamine
Therapeutic Uses |
Epinephrine reversal
HTN Reversal of the ischemia and tissue necrosis c/b extravasation of dopamine Pheochromocytoma Erectile dysfunction |
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Phentolamine
Adverse Reaction |
1. Orthostatic hypotension
2. Angina 4. Failure to ejaculate/retrograde ejaculatin 5. Miosis (unopposed PNS) 6. Nasal congestion (unopposed PNS) 7. Abdominal cramping (unopposed PNS) |
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Doxazosin
MOA |
a-antagonist
a-blockers |
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Doxazosin
Pharm Effects |
CV effects in HTN w/ normal cardiac fxn: ↓ TPR & BP, ↑ venous capacitance; no effect on HR, dt/dt, or CO
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Doxazosin
Therapeutic Uses |
HTN
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Doxazosin
Adverse Reaction |
Same as phentolamine, except angina
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Labetalol
MOA |
a-antagonist
a-blockers also blocks B1 |
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Labetalol
Pharm Effects |
CV effects in hypertensive pts with normal cardiac fxn: ↓ TPR, BP, dp/dt; ↑ venous capacitance; 0/↓ HR; has
no effect on CO |
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Labetalol
Therapeutic Uses |
Hypertension; especially HTN emergency
Not effective in Pheochromocytoma preoperative BP control |
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Labetalol
Adverse Reaction |
Same as phentolamine, except for angina
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Ergotamine
MOA |
a-antagonist
a-blockers partial a-agonist |
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Ergotamine
Pharm Effects |
Believed to reduce pain by partial constriction of “dilated” cerebral blood vessels
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Ergotamine
Therapeutic Uses |
Migraine headache
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Ergotamine
Adverse Reaction |
Migraine tx S/E’s: spontaneous abortion, muscle pain, paresthesias, digital vasospasm, and gangrene
Same as phentolamine, except for angina |
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Betaxolol
“BAM” MOA |
B-blockers
Selective for β1 |
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Betaxolol
“BAM” Pharm Effects |
Cardioselectivity ++
Heart: blocks all B1 on left side of charts starting pg. 22 last section -↓ myocardial oxygen demand and coronary blood flow BP: the net effect is slow-developing decline in BP, even in pts who were normotensive prior to therapy Kidney: ↓ (JG cells) renin release 30-50% so plasma renin activity (PRA) & plasma Angiotensin II fall; in hypertensive pts, the 8-10 mmHg decline in BP caused by these drugs may cause salt & H2O retention & ECF volume expansion if filtration fraction is increased. Lungs: Increased airway resistance ↓ FEV1. Eye: local application to ↓ IOP by ↓ aqueous humor production via unknown mechanism (exception: propanolol) Metabolic effects: blocks lipolysis c/b sympathetic stimulation of adipocytes |
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Betaxolol
“BAM” Therapeutics Uses |
Cardiac dysrhythmias: most effective esp supraventricular arrhythmias, may also prevent the PVC’s c/ b the psychological stress; initiation of therapy soon after MI decreases the probability of subsequent sudden death by 25-40% probably by preventing fatal catecholamine-induced ventricular dysrhythmias.
Angina pectoris: reduces myocardial O2 demand & decreases the frequency of attacks, increases exercise tolerance, and reduces the need for nitroglycerin. Hypertension Hyperthyroidsim (Grave’s disease) Pheochromocytoma Glaucoma Migraine headache: fewer episodes; no beneficial effect after headache has begun. |
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Betaxolol
“BAM” Adverse Reaction |
Heart: depression of myocardial contractility (neg inotropic effect)
Bradycardia: contraindicated in AV block Up-regulation of B-blockers: sudden cessation of therapy can precipitate cardiac palpitations & tremor Lungs: large daily doses of the cardioselective B-blockers may also dec FEV1. Glucose metabolism in type 2 (non-insulin dep) DM: B-blockers do not prevent the insulin release elicited by the orally-acting hypoglycemic drugs like glipizide; despite this fact, the B-adrenoceptors are relatively contraindicated in Type 2 DM. Impotence: reversible/ mechanism unknown |
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Atenolol
“BAM” MOA |
B-blockers
Selective for β1 |
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Atenolol
“BAM” Pharm Effects |
Cardioselectivity ++
See Betaxolol Least decrease in FEV1 |
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Atenolol
“BAM” Therapeutic Uses |
Same as betaxolol
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Atenolol
“BAM” Adverse Effects |
Same as betaxolol
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Metoprolol
“BAM” MOA |
B-blockers
Selective for β1 |
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Metoprolol
“BAM” Pharm Effects |
Cardioselectivity +
See Betaxolol Least decrease in FEV1 |
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Metoprolol
“BAM” Therapeutic Uses |
Same as betaxolol
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Metoprolol
“BAM” Adverse Effects |
Same as betaxolol
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Esmolol
i.v. MOA |
B-blockers
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Esmolol
i.v. Pharm Effects |
Cardioselectivity +
t1/2 = 9 min |
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Esmolol
Therapeutic Uses |
Same as betaxolol
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Esmolol
Adverse Reaction |
Same as betaxolol
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Propranolol
MOA |
B-blockers
Non-selective (B1 & B2) |
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Propranolol
Pharm Effect |
1. No cardioselectivity
Lung: Most decrease in FEV1 Digits: Digital blood flow may be reduced significantly by non-selective antagonist Eye: Not used to reduce IOP b/c of its anesthetic effects which may reduce sensation of foreign bodies in the eye Metabolic: lypolysis, blocks glycogenolyis in liver and skeletal musc. |
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Propranolol
Therapeutic Uses |
Pheochromocytoma: used before and during surgery in combo with a-antagonist
Essential tremor: non-selective drugs are most effective (a portion of the tremor derives from peripheral B2 stimulation) Portal HTN: ↓ in CO c/b propranolol ↓ hepatic portal pressure and hemorrhage from esophageal varices |
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Propranolol
Adverse Reaction |
Up-regulation of B adrenoceptors: “propranolol withdrawal syndrome”
Lungs: contraindicated in COPD and chronic bronchitis b/c ↓FEV1 Glucose metabolism: Type 1: mask warning s/s of hypoglycemia, slows rate of recover of plasma glucose, produces severe HTN (d/t high plasma [ ] of epi) Digital blood flow may be reduced significantly by non-selective antagonist & pts complain of cold hands so they are contraindicated in Raynaud’s syndrome and Buerger’s dz; Smoking accentuates fall in digital blood flow. Exercise intolerance in nonanginal pts: non-selective agents block the increased FEV1, CO, & muscle blood flow caused by vigorous exercise |
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Timolol
MOA |
B-blockers
Non-selective (B1-B2) |
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Timolol
Pharm Effects |
No cardioselectivity
Most decrease in FEV1 |
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Timolol
Therapeutic Uses |
Pheochromocytoma: non selective B-blockers used before and during surgery in combo with a-antagonist
Essential tremor: an accentuation of the normal physiological tremor of 8-12 Hz that occurs in the absence of other neuro dysfunction; excess caffeine, lack of sleep, alcohol hangover, & strenuous can induce short bouts of tremor, but essential tremor is more persistent & impairs the ability of the pt to perform simple tasks such as writing, eating, & drinking; non-selective drugs are most effective (a portion of the tremor derives from peripheral B2 stimulation |
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Timolol
Adverse Reaction |
Digital blood flow may be reduced significantly by non-selective antagonist & pts complain of cold hands; they are contraindicated in Raynaud’s syndrome and Buerger’s dz; Smoking accentuates fall in digital blood flow.
Exercise intolerance in nonanginal pts: non-selective agents block the increased FEV1, CO, & muscle blood flow cuased by vigorous exercise |
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Alpha-methyldopa
MOA |
-Sympatholytic drug
-a-methyl-NE: stimulates α2-adrenoceptors= ↓ preganglionic sympathetic nerve activity -↓ SNS reduces the amount of NE and a-methyl-NE released from peripheral sympathetic fibers which innervate the ♥ & blood vessels. - Symp reflexes are attenuated but not blocked |
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Alpha-methyldopa
Pharm Effects |
Blood vessels dilate passively b/c SNS activity is decreased:
-dilation of arterioles = ↓ TPR & DBP -dilation of venules ↑ venous capacitance & thus lowers venous return = net effect is balanced vasodilation. Heart: the inc HR which occurs when moving from supine to standing position is attenuated, CO is unchanged or dec slightly, myocardial O2 demand is decresed Kidney: the dec in renal perfusion pressure may result in increased filtration fraction which slowly causes salt/H2O retention. Pituitary gland: Prolactin secretion increases. |
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Alpha-methyldopa
Therapeutic Uses |
Used to treat hypertension in kids and pregnant women (b/c it has less teratogenic effects on the fetus)
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Alpha-methyldopa
Adverse Effects |
Sedation and somnolence, dry mouth and nasal congestion, edema, flu-like syndrome, hepatitis and hyperprolactinemia (males may develop gynecomastia, oligospermia & impotence or dec libido; females can develop amenorrhea and galactorrhea)
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Cocaine
Alkaloid of botanical origin MOA |
-Local anesthesia: blocks Na channels in neuronal membranes of sensory pain fibers
-noncompetitive blockade of monoamine uptake1 transporter in central/periph neurons amplifies the postjunctional/ postsynaptic effects of NE, DA, Epi, & serotonin (5HT) -centrally increases peripheral sympathetic outflow -euphoria & addictive properties result from inc DA release in nucleus accumbens |
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Cocaine
Alkaloid of botanical origin Pharm Effects |
Local anesthesia
CNS: Euphoria. Very addicting Dose-related increase in BP & HR Vasoconstriction: -local application of cocaine produces intense vasoconstriction. -produces noncompetitive blockade of the uptake1 transporter, so NE released by normal symp nerve activity accumulates in the nerve junction. The increased NE concentration in the nerve junction causes persistent stimulation of postjunctional a-adrenoceptors in vascular smooth muscle: persistent vasoconstriction ensues. Local hemostasis: the intense vasoconstriction accounts for the hemostasis which occurs when cocaine is used as a topical anesthetic agent |
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Cocaine
Alkaloid of botanical origin Therapeutic Uses |
Local anesthesia in ocular and nasal surgery
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Cocaine
Alkaloid of botanical origin Adverse Reaction |
Cardiac dysrhythmias: blockade of Na channels impairs ventricular impulse conduction providing a substrate for re-entrant ventricular dysrhythmias; increases NE release (central effect) and potentiates the cardiac actions of NE (blockade fo uptake1)
MI Chest pain mimicking MI Pulmonary edema: results from a direct depressant effect on cardiac contractility and inc afterload CVA: Respiratory dz: barotrauma, pulmonary hemorrhage, & hypersensitivity pneumonitis Seizures Sudden death “Crack” burns of the larynx Necrosis of the nasal septum |
