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108 Cards in this Set

  • Front
  • Back
Nn
Ligand-gated cation channels; opening of an intrinsic cation channel; located on ganglionic neurons
Nm
Ligand-gated cation channels; opening of an intrinsic cation channel; located on skeletal neuro-muscular endplates
M1
Gq; increase PLC and IP3; closing K+ channels; located on ganglionic neurons
M2
Gi; decrease cAMP; opening of K+ channels; located in myocardium and presynaptic terminals
M3
Gq; increase PLC and IP3; closing K+ channels; located on smooth muscle, exocrine glands, vascular endothelium
Alpha1
Gq; increase PLC and IP3; increase eicosanoids; located on vascular and visceral smooth muscle
Alpha2
Gi; decrease cAMP; opening of K+ channels; located on some presynaptic terminals
B1
Gs; increase cAMP; closing of K+ channels; located on myocardium and JG cells
B2
Gs; increase cAMP; closing of K+ channels; located on visceral and vascular smooth muscle
B3
Gs; increase cAMP; closing of K+ channels; located on adipocytes
D1
Gs; increase cAMP; located on vascular smooth muscle
D2
Gi; opening of K+ channels, blocking of Ca+2 channels; located on presynaptic terminals
Muscarinic Agonists (choline esters)
Ach
Carbachol
Bethanechol
Muscarinic Agonists (natural alkoids)
Pilocarpine
Muscarine
AchEsterase Inhibitors (reversible)
Edrophonium
Physostigmine
Neostigmine
Donepezil
AchEsterase Inhibitors (irreversible)
Parathion
(Organophosphates)
AchEsterase Inhibitors (reactivators)
Pralidoxime
AntiMuscarinics (tertiary amines)
Atropine
Scopolamine
Homatropine
Darifenacin
Benztropine

*All can enter the CNS!
AntiMuscarinics (quaternary NH4 compounds)
Glycopyrrolate
Ipratropium
Ganglionic Stimulants
Nicotine
Ganglionic Blockers
Mecamylamine
Alpha & Beta Agonists
Epinephrine
Norepinephrine
D1 & D2 Agonists
Dopamine
Alpha1 Agonists
Phenylephrine
Alpha2 Agonists
Clonidine
Apraclonidine
Tizanidine
Nonselective B Agonists
Isoproterenol
B1 Agonists
Dobutamine
B2 Agonists
Albuterol
Salmeterol
Mixed-Acting Adrenergics (indirect)
Tyramine
Methyldopa
Amphetamines
Cocaine
Nonselective Alpha Blockers
Phenoxybenzamine
Alpha1 Blockers
Prazosin
Tamsulosin
B1 Blockers
Atenolol
Metoprolol
Esmolol
Nonselective B Blockers
Pindolol
Propranolol
Sotalol
Timolol
Alpha & Beta Blockers
Labetalol
Adrenergic Blockers (indirect)
Metyrosine
Cholinergic receptor of HEART and actions
M2; decrease in heart rate, contractility, and velocity; no effect on the ventricle
Cholinergic receptor of ARTERIOLES and actions
M3 (via NO); dilation; no innervation therefore no effect by indirect agonists
Cholinergic receptor of LUNG and actions
M3; bronchial muscle contraction; increased secretions
Cholinergic receptor of EYE and actions
M3; contraction of the sphincter of iris (miosis) and ciliary muscle (accommodation of near vision); increased secretions
Cholinergic receptor of GI and actions
M3; increased motility and tone; increased secretions; relaxation of the sphincters EXCEPT for the LES
Cholinergic receptor of PANCREAS and actions
M3; increased insulin secretion
Cholinergic receptor of BLADDER and actions
M3; contraction of detrusor muscle; relaxation of the trigone and sphincter; voiding and urinary incontinence
Adrenergic receptor of HEART and actions
B1; increased HR, force of contraction, automaticity, and conduction velocity (both atria and ventricles)
Adrenergic receptor of ARTERIOLES and actions
A1 = constriction; various organs, skin, GI, and GU
B2 = dilation; skeletal muscle and liver
Adrenergic receptor of LUNG and actions
B2; relaxation of bronchial muscles; decreased secretions
Adrenergic receptor of PLATELETS and actions
A2; aggregation
Adrenergic receptor of FAT CELLS and actions
B3; increased lipolysis
Adrenergic receptor of PANCREAS and actions
A2; decreased insulin secretion
B2; increased insulin secretion
Adrenergic receptor of LIVER and actions
B2; increased glycogenolysis and gluconeogenesis
Adrenergic receptor of GI and actions
A1; contraction of sphincters
Adrenergic receptor of KIDNEY and actions
B1; increased renin release
Adrenergic receptor of BLADDER and actions
A1; contraction of trigone and sphincter
B2; decreased motility and tone
Adrenergic receptor of EYE and actions
A1; contraction of the radial muscle (mydriasis)
A2; decreased aqueous humor production from the ciliary epithelium
B2; increased aqueous humor production from the ciliary epithelium
Therapeutic uses of EPI
Serious acute hypersensitivity reactions (anaphylaxis, angioedema); prevention of surgical bleeding; to retard the absorption of local anesthetics; asthma; glaucoma; cardiopulmonary resuscitation in cardiac arrest
Adverse effects of EPI
CNS: fear, anxiety, throbbing headache, dizziness, tremors
CV: HTN, palpitations, sinus tachycardia, pulmonary edema
Contraindications of EPI
HTN, hyperthyroidism, angina, cardiac arrhythmias, shock, diabetes
Therapeutic uses of NORE
Hypotension and vasodilatory shock due to spinal trauma, spinal anesthesia, and sepsis; with local anesthetics to retard absorption
Therapeutic uses of Dopamine
Some types of cardiogenic, neurogenic, and septic shock when poor renal perfusion is suspected
Therapeutic uses of Phenylephrine
Postural hypotension, nasal decongestants, mydriatics, local vasoconstrictors
Adverse Effects of Phenylephrine
HTN, anginal pain, rebound congestion, photophobia
Contraindications of Phenylephrine
HTN, cardiac diseases, hyperthyroidism, urinary retention
Therapeutic uses of Clonidine
HTN (2nd choice), withdrawal from tobacco, alcohol, and opioids, neuropsychiatric disorders
Therapeutic uses of Apraclonidine
Glaucoma
Adverse effects of A2 selective agonists
Overt sedation, drowsiness, nightmares, xerostomia, sexual dysfunction
Therapeutic uses of Isoproterenol
Emergency situations where heart contractility is low and heart rate is slow, yet TPR is high; poymorphic ventricular tachycardia (torsade de pointes); beta blocker overdose
Therapeutic uses of Dobutamine
Cardiogenic shock, IV infusion
Therapeutic uses of Albuterol and Salmeterol
Albuterol = Intermediate acting
Salmeterol = Long acting
Asthma, COPD, premature labor, hyperkalemia
Adverse effects of B2 agonists
CNS - tremor, restlessness;
CV - sinus tachycardia, palpitations, hypotension, arrhythmias, angina
Other - hypokalemia, hyperglycemia
Contraindications of B2 agonists
Cardiac arrhythmias, CAD, hyperthyroidism, pheochromocytoma, diabetes
Therapeutic uses of Phenoxybenzamine
Pheochromocytoma
Therapeutic uses of Prasozin and Tamsulosin
Urological problems: BPH and overflow incontinence; Raynaud's disease; chronic HTN
Adverse effects of A antagonists
CV: postural hypotension, tachycardia, palpitations, cardiac arrhythmias;
CNS - fatigue, dizziness, drowsiness;
GI - nausea, vomiting, diarrhea or constipation;
Other - urinary frequency, urinary incontinence, sexual dysfunction
Contraindications of A antagonists
Urge incontinence, exertional angina, postural hypotension
Local anesthetic action
Propranolol, Pindolol, Metoprolol
Pronounced K+ channels blocking activity
Sotalol
Parenteral administration only (short half-life)
Esmolol, used during surgery
Partial beta-agonist activity
Pindolol
Therapeutic uses of B antagonists
Main uses - HTN, cardiac arrhythmias, exertional angina;
Other - glaucoma, hyperthyroidism, acute MI, chronic heart failure, tremor, migraine headache, social phobias
Adverse effects of B antagonists
CNS - insomnia, dizziness, nightmares;
GI - nausea, vomiting, diarrhea;
Other - sexual dysfunction, increased probability of hypoglycemic reactions, hypertensive crisis, hyperkalemia
Contraindications of B antagonists
Abrupt discontinuation; asthma, bronchitis, COPD; diabetes, depression
Adverse effects of Ach and Carbachol
When given locally on the conjuctiva - visual difficulty with far vision or in dim light; reddening, stinging, and burning of the conjuctiva
Adverse effects of Bethanechol
When given systemically - nausea, vomiting, abdominal pain, diarrhea; bronchospasm; sweating, lacrimation, salivation; urinary urgency; hypotension
Contraindications of Ach and Carbachol
Iritis, cataracts
Contraindications of Bethanechol
Asthma, COPD; cardiac arrhythmias, CAD; peptic ulcer disease, GI obstruction, IBS; urinary tract obstruction; hyperthyroidism
Therapeutic use of Bethanechol
Paralytic ileus and urinary retention
Therapeutic use of Carbachol
Glaucoma
Adverse effects of Cholinergic Natural Alkaloids
Pilocarpine and Muscarine can enter the CNS; poisoning produced by muscarine containing mushrooms - develop within 30-60 minutes of ingestion and include salivation, lacrimation, sweating, nausea, vomiting, visual disturbances, bradycardia, hypotension, tremors, and coma
Therapeutic use of Pilocarpine
Glaucoma and xerostomia
Toxicity of AchE Inhibitors
Acute poisoning - signs and symptoms appear within 5-10 minutes after inhalation, or within 30-60 minutes after GI or percutaneous absorption; death is mainly due to primary respiratory failure; Treatment - administration of atropine; administration of AchE reactivators (Pralidoxime) in case of poisoning by organophosphates
Contraindications of AchE Inhibitors
GI and urinary tract obstruction; cholinergic crisis in myasthenia patient; asthma, COPD; hypotension, cardiac arrhythmias, CAD; peptic ulcer disease; hyperthyroidism; seizure, Parkinson disease
Therapeutic use of Donepezil
Alzheimer disease
Therapeutic use of Edrophonium
Diagnosis of myasthenia; differential diagnosis between myasthenia and cholinergic crisis
Therapeutic use of Physostigmine
Glaucoma; antidote in Atropine overdose
Therapeutic use of Neostigmine
Myasthenia; postoperative and postpartum urinary retention; neurogenic bladder; postoperative nonobstructive ileus
Therapeutic use of Parathion (and other organophosphates)
Glaucoma; insecticides
Toxicity of Antimuscarinic drugs
Acute poisoning - Atropine can be lethal in children, signs and symptoms appear within 30-60 minutes after ingestion, death is due to respiratory failure; treat with Physostigmine
Contraindications of Antimuscarinic drugs
Glaucoma, prostatic hypertrophy, urinary tract or GI obstruction, ulcerative colitis, Crohn's disease, CAD, hyperthyroidism, children, elderly
Therapeutic use of Atropine
Excessive salivation, cardiovascular disorders, AcheE inhibitor overdose, ophthalmology, preanesthetic medication
Therapeutic use of Scopolamine
Motion sickness, ophthalmology, preanesthetic medication
Therapeutic use of Homatropine
Ophthalmology
Therapeutic use of Darifenacin
Neurogenic bladder, urinary urge incontinence
Therapeutic use of Benztropine
Parkinson's disease
Therapeutic use of Glycopyrrolate
Visceral hypermotility and spasms, cardiovascular disorders, preanesthetic medication
Therapeutic use of Ipratropium
Bronchospastic disorders
Therapeutic use of Nicotine
Treatment of nicotine addiction
Acute Nicotine Poisoning
Onset of symptoms is rapid - salivation, nausea, vomiting, abdominal pain, diarrhea, cold sweat, tachypnea, tachycardia, headache, dizziness, mental confusion, marked weakness; death may result within few minutes from respiratory failure
Therapeutic use of Mecamylamine
Tourette's syndrome; ganglion blocking drugs like mecamylamine prevent baroreceptor reflex changes in heart rate elicited by vasoconstriction (A1) and vasodilation (B2)
Treatment for Thryotoxicosis
Propanolol is the only B-blocker used for hyperthyroidism; it also has sedative effects