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PHAR 420

Neuropharmacology and Medicinal Chemistry

ResponseReceptor
Accommodation for near vision alpha1
Aggravation of closed angle glaucoma alpha1
Contracts urinary sphincters alpha1
Ejaculation alpha1
Increased glycogenolysis alpha1, beta2
Increased salivation alpha1, M3
Increased localized sweating alpha1
Mydriasis (pupil dilation) alpha1
Piloerection alpha1
Contraction of GI sphincters alpha2
Decrease insulin secretion alpha2
Decrease synthesis of aqueous humor alpha2
Decreased NE release alpha2
Increased peripheral resistance alpha2
Increased renin secretion beta1
Increased renal blood flow beta1
Increased force of contraction of the heart beta1, beta2 (minor)
Positive chronotropy (increased HR) beta1
Positive dromotropy (increased conduction velocity) beta1
Decongestion beta2
Decreased nasal secretions beta2
Decreased uterine contractions beta2
Hypokalemia during stress beta2
Relaxation of ciliary muscle for near vision beta2
Vasodilation of skeletal muscle blood vessels beta2
Bronchodilation beta2
Activation of lipolysis beta3
Contraction of bladder detrusor muscle beta3
Decrease force of contraction of the heart M2
Decreased conduction through cardiac AV node M2
Negative inotropy (decreased contractility) M2
Negative chronotropy (decreased HR) M2
Bronchoconstriction M3
Increased gastric secretions M3
Increased urination M3
Increased GI motility M3
Increased thermoregulatory sweating M3
Miosis (constriction of pupil) M3
Autonomic ganglionic transmission Nn
Secretion of EPI from adrenal medulla Nn
Increased contractility of skeletal muscle beta2
What neurotransmitter(s) is used in the preganglionic parasympathetic system? Acetylcholine
What neurotransmitter(s) is used in the preganglionic sympathetic system? Acetylcholine
What neurotransmitter(s) is used in the postganglionic parasympathetic system? Acetylcholine
What neurotransmitter(s) is used in the postganglionic sympathetic system? Acetylcholine, norepinephrine, dopamine
What neurotransmitter(s) is used at the adrenal medulla? Epinephrine, norepinephrine
What neurotransmitter(s) has sympathetic innervation of renal blood vessels? Dopamine
Why is there a widespread response in sympathetic nervous system and a local effect in parasympathetic nervous system? Adrenergic receptors of sympathetic division respond to adrenal gland secretions. Circulating adrenalin disperses to many glands.
True/False: Parasympathetic nerves innervate blood vessels? False
What brain center regulates heart beat and breathing? Medulla oblongata
How does the central nervous system regulate the autonomic nervous system? Acetylcholine activates nicotinic receptors and epinephrine and norepinephrine is released. Norepinephrine is converted to epinephrine by PNMT and stored in chromaffin granules.
What does choline acetyltransferase do? Acetylcholine biosynthesis
How is epinephrine made from tyrosine? Tyrosine ---tyrosine hydroxylase---> DOPA ---DOPA decarboxylase---> dopamine ---dopamine beta hydroxylase---> norepinephrine ---phenylethanolamine N-methyltransferase---> epinephrine
Where does MAO metabolism occur? Nerve terminal, liver (after diffusion from synapse)
Where does COMT metabolism occur? Postsynaptic tissue
How would you increase the levels of acetylcholine in cholinergic synapse? Non-depolarizing blocking agents (Tubocurarine), anticholinesterases (Neostigmine)
How would you decrease the levels of norepinephrine in adrenergic synapse? Reserpine, alpha-methyltyrosine
Is phenylethylamine a catecholamine? No
Is epinephrine a catecholamine? Yes
Is norepinephrine a catecholamine? Yes
Is dopamine a catecholamine? Yes
Is phenylephrine (Neosynephrine) a catecholamine? No
Is Dobutamine a catecholamine? Yes
Is Tertbutaline a catecholamine? No
True/False: Non-catecholamines have higher bioavailability than catecholamines. True
True/False: By crossing the blood brain barrier, metabolism by MAO and COMT is decreased. True
What kind of drug would you recommend for nasal congestion? alpha1 agonist
What are two drugs that can be used for nasal congestion? Phenylephrine (Neosynephrine) and Oxymetazoline
Explain why MAOIs are contraindicated with alpha1 agonists? MAOI increase levels of epinephrine and there is an additive effect on blood vessels.
What is Clonidine's mechanism of action in reducing blood pressure? It decreases sympathetic neurotransmitter outflow from brainstem and decreases norepinephrine release from parasympathetic nervous system.
What is Clonidine's mechanism of action in ADHD? Acts on postsynaptic alpha2 receptors in prefrontal coretex. Decreases neurotransmitters which increases cognitive function.
What is Clonidine's mechanism of action in pain management? It decreases neurotransmitter release from pain fiber, and suppresses pain transmission from dorsal horn.
True/False: Clonidine can result in withdrawal symptoms if discontinued abruptly. True
What is the preferred drug treatment for hypertension during pregnancy? Methyldopa
What are contraindications for Methyldopa? Liver disease and hemolytic anemia
What drugs are indicated for open angle glaucoma? Apraclonidine and Brimonidine
What does Dobutamine do? It is a beta1 agonist and a catecholamine. It will increase cardiac output.
What is epinephrine's mechanism of action with bradycardia? Acts on beta1 and increases heart rate.
Why should patients with angina/MI be treated cautiously with epinephrine? Epinephrine increases heart rate which increases workload and oxygen demand.
What drug should be used for extravasation with epinephrine use? An alpha1 blocker Phentolamine.
What is the advantage of using dopamine over norepinephrine in cardiogenic shock treatment? Dopamine causes vasodilation of renal blood vessels maintaining flow to kidneys.
What is Bromocriptine? Dopamine agonist that causes inhibition of pituitary gland and decreases prolactin.
What is Bromocriptine used for? Acromegaly, Parkinson's, type II diabetes, hyperprolactinemia
What are two indications for methylphenidate and amphetamines? Narcolepsy and obesity
Is amphetamine a direct or indirect acting adrenergic drug? Indirect
Is phenylephrine a direct or indirect acting adrenergic drug? Direct (alpha1)
Is Albuterol a direct or indirect acting adrenergic drug? Direct (beta2)
Is Atomoxetine a direct or indirect acting adrenergic drug? Indirect (NE reuptake inhibitor)
What is Lisdexamphetamine (Vyvanse)? Prodrug of d-amphetamine
What are the advantages of Concerta (methylphenidate)? Once daily dosing and privacy of home.
What are the advantages of Lisdexamphetamine (Vyvanse)? Once daily dosing and low abuse potential.
What are the advantages of Atomoxetine (Strattera)? It's not controlled, no anxiety or insomnia, and no addiction.
What are the adverse drug reactions of Atomoxetine (Strattera)? Suicidal idealation, liver toxicity
What are the advantages of using Clonidine and guanfacine as alternative agents to amphetamine and methylphenidate in the treatment of ADHD? Useful in anxiety and insomnia patients, and no appetite suppression.
What is Modafinil's mechanism of action? Inhibits dopamine and norepinephrine reuptake
What is Modafinil used for? Narcolepsy, sleep apnea, sleep work shift disorder
What are the adverse effects of Methamphetamine? Xerostomia and rampant caries
What are the adverse effects of Cocaine? Ischemia of fingers, toes and kidneys, and hyperthermia
What is Metaraminol and what is it used for? It's an alpha1 agonist and used for hypotension.
Created by: sdeck86