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PHAR 420
Neuropharmacology and Medicinal Chemistry
| Response | Receptor |
|---|---|
| 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
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