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96 Cards in this Set
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Ciliary Muscle Receptors
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Muscarinic(M;contract muscle- for near focus)and Beta 2 adrenergic (Beta 2; relax muscle- for far focus) receptors
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parasympathetic and sympathetic
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Vascular Smooth Muscle Receptors
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Alpha1 (contract)and Beta2 (relax) adrenergic receptors
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just sympathetic
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Sinoatrial Node Receptors
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Muscarinic (decreased HR; bradycardia) and Beta1 (and some Beta2) adrenergic (increased HR; tachycardia) Receptors
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parasympathetic and sympathetic
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Gastrointestinal Smooth Muscle receptors
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Muscarinic (contraction) and Beta2 adrenergic (relaxation) receptors
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parasympathetic and sympathetic
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Bronchial Smooth Muscle Receptors
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Muscarinic (contraction) and Beta2 adrenergic (relaxation) receptors
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parasympathetic and sympathetic
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Sphincter (colonic, esophageal and urinary bladder) Muscle Receptors
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Muscarinic (relaxation) and Alpha1 adrenergic (contraction) receptors
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parasympathetic and sympathetic
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Urinary Bladder Detrusor Muscle Receptors
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Muscarinic (contraction) and Beta2 adrenergic (relaxation)
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parasympathetic and sympathetic
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Urethral Receptors
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Muscarinic (relaxation) and Alpha 1 adrenergic (contraction) receptors
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parasympathetic and sympathetic
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Salivary Gland Receptors
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Muscarinic (increased thin watery secretion, copious) and Alpha1 adrenergic (increased mucous secretion, thick)
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parasympathetic and sympathetic
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Pupil Smooth Muscle Receptors
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Muscarinic (contraction circular muscle; constricts pupil; miosis) and Alpha1 adrenergic (contraction radial muscle; dilates pupil; mydriasis)
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parasympathetic and sympathetic
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Norepinephrine Degrading Enzymes (name, location and inhibitors)
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Monoamine Oxidase (MAO, mitochondrial outer membrane, phenelzine) and Catechol-O-methyltransferase (COMT, cytoplasm, tolcapone)
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2
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Acetylcholine Degrading Enzyme (name, location and inhibitors)
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Acetylcholinesterase (AChE, postsynaptic membrane, organophosphates)
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Alpha Adrenergic Receptor agonist potency
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E >,= NE >> isoproterenol
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Beta1 Adrenergic Receptor agonist potency
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isoproterenol > E = NE
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Beta2 Adrenergic Receptor agonist potency
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isoproterenol > E >> NE
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Alpha1 Adrenergic Receptor
Signal Transduction |
Increases IP3 and DAG
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Increase Phospholipase C
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Beta Adrenergic Receptors Signal Trasduction
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Increase cAMP
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activates Gs
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Alpha2 Adrenergic Receptor Signal Transduction
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Decrease cAMP
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activates Gi
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adrenergic drugs that pass through the BBB
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Reserpine and alpha-methyltyrosine
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2
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alpha2 selective agonists
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clonidine and alpha-methylnorepinephrine (both CNS action)
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2
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Nonselective (alpha, beta) adrenergic agonists
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epinephrine
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1
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Alpha1 selective agonists
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phenlyephrine
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1
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Beta selective agonists
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isoproterenol
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1
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Beta1 selective agonists
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dobutamine
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1
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Beta2 selective agonists
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albuterol
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1
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Nonselective (alpha1, beta1,2) antagonists
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carvedilol
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1
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Alpha selective antagonists
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phentolamine (competitive antagonist; shorter acting-hours) and phenoxybenzamine (irreversible antagonist; longer acting-days)
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2
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Alpha1 selective antagonists
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prazosin
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1
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Beta selective antagonists
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propranolol
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1
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Beta1 selective antagonist
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metoprolol
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1
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Ganglionic blocker
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mecamylamine
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1
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TH inhibitor
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alpha-methyltyrosine
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1
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DA analog
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alpha-methyldopa
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1
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Adrenergic vesicular uptake inhibitor
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reserpine
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1
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Adrenergic reuptake inhibitors
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cocaine and imipramine
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2
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Indirectly acting sympathomimetics
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D-amphetamine (and tyramine)
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1 (and 1)
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mixed-acting sympathomimetics
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ephedrine
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1
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Choline Esters
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bethanechol and carbechol
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2
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Reversible Acetylcholinesterase Inhibitors
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edrophonium, neostigmine, physostigmine, and pyridostigmine
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4
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Irreversible Acetylcholinesterase Inhibitors
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echothiophate(organophosphate)
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1
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reverses acetylcholinesterase inhibition by an 'irreversible' AChE inhibitor
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pralidoxime
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1
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Cholinergic nerve blocker
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botulinum toxin
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1
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Muscarinic Receptor Antagonists
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atropine, ipratropium, scopolamine
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3
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Beta1 adrenergic receptor agonists -action
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increase heart output
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Where are the receptors concentrated?
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Beta1 adrenergic receptor antagonists- action
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prevent increase in heart output by Beta1 agonists
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Where are the receptors concentrated?
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Beta2 adrenergic receptor agonists- action
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open (dilate) airways
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Where are the receptors concentrated?
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Beta2 adrenergic receptor antagonists- action
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constrict airways
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Where are the receptors concentrated?
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Alpha1 adrenergic receptor agonists- action
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constrict vessels, increase BP
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Where are the receptors concentrated and usually dominant?
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Alpha1 adrenergic receptor antagonists- action
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dilate vessels, decrease BP
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Where are the receptors concentrated and usually dominant?
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ganglionic blockers- example, uses, side effects and contraindications
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example: mecamylamine
uses: rapid pressure reduction in acute dissecting aortic aneurysm and clinical management of hyperreflexia side effects: paralytic ileus, urinary retention, respiratory arrest and syncope. contraindications: coronary insufficiency and glaucoma |
blocks both parasympathetic and sympathetic outflow- effect on organ will be the blockade of the predominat tone of that organ.
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alpha-methyltyrosine- action, uses
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action: competitive inhibitor of TH
uses: in treatment of pheochromocytoma prior to surgery or when surgery is not feasible |
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alpha-methyldopa- action, uses
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action: crosses BBB, DOPA analog- prodrug converted to alpha-methylnorepinephrine- agonist at Alpha2 adrenergic receptors in CNS
uses: treat hypertension |
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reserpine- action, uses, side effects
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action: irreversible blocking vesicular uptake of catecholamines
uses: original use as an antihypertensive- but side effects too great!!! side effects: cardiac arrhythmia; crosses BBB- so CNS side effects too |
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Imipramine- action, uses
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action: Reuptake inhibitor
uses: to treat enuresis- by increasing sympathetic tone of bladder sphincter and relaxation of bladder wall. |
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amphetamine- action, uses, side effects and contraindications
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action: indirect acting sympathomimetic
use: treatment of ADHD, narcolepsy and appetite suppression side effects: tachycardia and hypertension contraindications: severe hypertension, glaucoma, hyperthyroidism and MAOI therapy- also do not take during pregnancy- adverse effects on fetal development. |
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ephedrine- action, uses and contraindications
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action: mixed acting sympathomimetic
uses: asthma (bronchodilator) and nasal decongestant, also used as a pressor agent during epidural or intra-anesthesia side effects: tachycardia and hypertension contraindications: severe hypertension, glaucoma, hyperthyroidism and MAOI therapy. |
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clonidine and alpha-methylnorepinephrine- action, uses, side effects
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action: alpha-2 adrenergic receptor agonists
uses: centrally acting antihypertensives peripheral side effects: bradycardia, heart failure. |
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epinephrine- action, uses, contraindications
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action: adrenergic receptor agonist
uses: relieve respiratory distress due to bronchospasm, to ease hypersensitivity reactions (anaphylactic shock), used in cardiac arrest (increase heart rate (Beta1), and systolic pressure (Alpha2) and decreases some peripheral vascular resistance (Beta2), also used to prolong action of local anesthetics by local restriction of blood flow (Alpha1) contraindications: don't give in presence of Beta adrenergic receptor blockade (would lead to severe hypertension and cerebral hemorrhage), also contraindicated in narrow angle glaucoma. |
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phenylephrine-action, uses, side effects and contraindications
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action: alpha1 selective agonist
uses: treatment of shock, hypotension (inc BP by contricting BV) and as a nasal decongestant(decrease blood flow to nasal mucosa decreases mucous production) side effects: bradycardia and hypertension contraindications: glaucoma, hypertension hyperthyroidism, difficulty urinating (enlarged prostate gland) |
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albuterol- action, uses, side effects, contraindications
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action: Beta2 selective adrenergic receptor agonist
uses: treatment of asthma (dilation of airways), COPD side effects: tachycardia contraindications: cardiac disease (preexisting arrhythmias), hyperthyroidism |
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dopamine- peripheral uses
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uses: DOC for treatment of shock
used in the treatment of conditions characterized by compromised renal function- like shock- it dilates renal blood vessels. |
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prazocin- action, uses, side effects
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action: Alpha1 selective adrenergic receptor antagonist
uses: treatment of hypertension side effects: orthostatic hypotension |
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phentolamine and phenoxybenzamine- action, uses, side effects, and contraindications
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action: alpha selective adrenergic receptor antagonists (competitive and irreversible, respectively)
uses: in the treatment of pheochromocytoma, sometimes useful in the treatment of Raynaud disease. side effects: postural hypotension contraindications: don't use in patients with decreased coronary perfusion |
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propranolol-action, uses, side effects and contraindications
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action: Beta adrenergic receptor antagonist
uses: treatment of hypertension, angina, performance anxiety, hyperthyroidism, glaucoma (dec secretion of aqueous humor) side effects: bronchospasm, AV-block and bradycardia contraindications: bronchial asthma, COPD and bradycardia |
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metoprolol-action, uses, side effects and contraindications
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action: Beta1 selective adrenergic receptor antagonist
uses: angina, heart failure(decrease heart output), hypertension side effects: bronchospasm, atrioventricular block contraindications: asthma, sinus bradycardia |
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carvedilol
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action: nonslective adrenergic receptor antagonsist (alpha1, Beta1 and Beta2)
uses: treatment for congestive heart failure, hypertension |
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What is the rate limiting step in acetylcholine synthesis?
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Choline uptake
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LUSHPADS BBB
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Lacrimation
Urination Salivation Hypotension Pinpoint pupils Accomodation Defecation Sweating Bronchial contriction Bonchial secretion Bradycardia |
muscarinic effects of acetylcholine
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DUMBELS
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Diarhea
Urination Miosis Bronchial constriction/secretion Excitation (skeletal muscle and CNS) Lacrimation Sweating/salivation |
acetylcholine effects
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Direct Cholinomimetics
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Choline esters: bethanocol and carbachol
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2
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Indirect Cholinomimetics
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Acetylcholinesterase inhibitors
Reversible: edrophonium, neostigmine, physiostigmine, pyridostigmine Irreversible (organophosphate): echothiophate |
Acetylcholinesterase inhibitors
4 reversible 1 irreversible |
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Reverses 'irreversible' acetylcholinesterase inhibition
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pralidoxime
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1
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Cholinergic Nerve Blocker
(blocks Ach release) |
Botulinum toxin
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1
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Muscarinic Receptor Anatagonists
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atropine, ipatropium, scopolamine
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3
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Carbachol- action, uses, side effects
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action: Direct cholinomimetic-choline ester - resistant to hydrolysis by acetylcholinesterase.
uses: wide angle glaucoma, narrow angle glaucoma- treatment immediately prior to surgical iridotomy, cause pupil constriction (miosis) for eye surgery. side effects - are reduced due to local application and poor absorption profile (quaternary amine) |
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Bethanechol-action, uses, side effects and contraindications
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action: Direct cholinomimetic-choline ester- highly resistant to acetylcholinesterase and highly selective for muscarinic receptors-
uses: for treatment of urinary retention side effects: LUSHPADS BBB contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction |
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Edrophonium-action, uses
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action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor short half-life of inhibition (10-20 min)
uses: diagnosis of Myesthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine) |
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Neostigmine- action, uses, side effects, contraindications,
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action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor- intermediate half-life of inhibition (30min-2hrs)
uses: treatment of Myasthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine), alleviate smooth muscle atony of gastrointestinal and urinary tract. side effects: LUSHPADS BBB contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction, don't use when using succinylcholine for depolarization blockade during surgery |
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Pyridostigmine-action, uses
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action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor- intermediate half-life of inhibition (3 to 6 hrs)
uses: treatment of Myasthenia Gravis, reversal of pharmacologically induced neuromuscular block from competitive blockade (tuboburarine) not depolarization blockade (succinylcholine), alleviate smooth muscle atony of gastrointestinal and urinary tract. |
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Physiostigmine- action, uses, side effects, contraindications
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action: Indirect cholinomimetic- reversible acetylcholinesterase inhibitor-intermediate half-life of inhibition.
(Can gain access to CNS since not a quaternary amine) uses: wide angle glaucoma (local application), treat GI or urinary atony (increases motility), also to treat antimuscarinic toxicity and other drugs that have antimuscarinic effects side effects: LUSHPADS BBB contraindications: peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction, don't use when using succinylcholine for depolarization blockade during surgery |
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Echothiophate-action, uses
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action: Indirect Cholinomimetic- organophosphate-irreversible acetylcholinesterase inhibitor -long half-life of inhibition.
uses: treatment of wide angle glaucoma, treatment of strabismus |
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Pralidoxime- action, uses
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action: reverses 'irreversible' acetylcholinesterase inhibitor
note: also has some action as an inhibitor of acetylcholinesterase- so don't use with a non-organophosphate acetylcholinesterase inhibitor- would potentiate effect. uses: in the treatment of organophosphate toxicity |
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Side effects of cholinomimetics:
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LUSHPADS BBB
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Contraindications of cholinomimetics:
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peptic ulcer, asthma, coronary insufficiency, hyperthyroidism, gastrointestinal/urinary tract obstruction
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Acetylcholinesterase inhibitors are contraindicated when-
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using succinylcholine for depolarization blockade during surgery
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Botulinum Toxin-action, uses
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action: Cholinergic nerve blocker- blocks release of acetylcholine from nerve terminal
uses: treament of spasm of the eyelid, larynx, used for facial paralysis, cosmetics, and to prevent profuse sweating |
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Atropine-action, uses, side effects,
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action: muscarinic receptor antagonist
uses: preoperative medication to reduce salivation and respiratory secretions, to reverse bradycardia, treat spastic disorders of the GI and urinary tracts, in the treatment of organophosphate poisoning, to treat muscarine poisoning side effects: reverse of LUSHPADS BBB |
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Scopolamine-action, uses, side effects, contraindications
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action: muscarinic receptor antagonist
uses: motion sickness (CNS action) side effects: reverse of LUSHPADS BBB contraindications: narrow angle glaucoma, prostatic hypertrophy, cardiac disease, |
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Ipatropium-action, uses,
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action: muscarinic receptor antagonist
uses: asthma- decreases both watery and mucous secretions, COPD side effects reduced due to the fact that its a qauternary amine that given directly to lungs by inhalation- |
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Non-depolarizing Neuromuscular Blockers-names and uses
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names:tubocurarine, pancuronium, vecuronium, rocuronium
uses: relax muscles during surgery |
4
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Depolarizing Neuromuscular Blockers-names and uses
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name:succinylcholine
uses: when rapid endotracheal intubation is required, also used during elctroconvulsive shock treatment |
1
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Neuromuscular Blocker- block Ach release from terminal
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botulinum toxin
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1
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Stimulate release of Ach from neuromuscular junction
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4-aminopyridine
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1
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Spasmolytic drugs
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baclofen, diazepam, cyclobenzaprene, dantrolene
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4
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Isoproterenol-action, uses
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action: beta selective adrenergic receptor agonist
uses: rarely used as a bronchodilator in asthma, can be used to stimulate the heart in emergency situations |
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dobutamine-action, uses, contraindications
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action: Beta1 selective adrenergic receptor agonist
uses: increase cardiac output in congestive heart failure contraindications- should be used with caution with atrial fibrillation |
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