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