Term
List two clinical uses of norepinephrine. |
|
Definition
Hypotension, pressor agent. |
|
|
Term
What receptors does norepinephrine primarily bind to? |
|
Definition
|
|
Term
Does norepinephrine circulate? |
|
Definition
No. It is released by neurons. |
|
|
Term
List two types of drugs that interact with norepinephrine. |
|
Definition
Monoamine oxidase inhibitors and tricyclic antidepressants. |
|
|
Term
What is the drug of choice for allergic reactions? |
|
Definition
|
|
Term
What receptors does epinephrine interact with? |
|
Definition
|
|
Term
Does epinephrine circulate? |
|
Definition
Yes. It is released by the adrenal medulla into the circulation. |
|
|
Term
List two classes of drugs that epinephrine interacts with. |
|
Definition
Monoamine oxidase inhibitors and tricyclic antidepressants. |
|
|
Term
What is the drug of choice for shock? |
|
Definition
Norepinephrine (dopamine is a close second). |
|
|
Term
What receptors does dopamine bind to? |
|
Definition
|
|
Term
What drug is a precursor for norepinephrine? |
|
Definition
|
|
Term
What class of drug interacts with dopamine? |
|
Definition
Monoamine oxidase inhibitors. |
|
|
Term
List two uses of isoproterenol. |
|
Definition
Asthma, cardiac stimulant. |
|
|
Term
What receptors does isoproterenol interact with? |
|
Definition
|
|
Term
Is isoproterenol synthetic or endogenous? |
|
Definition
|
|
Term
What is the effect of isoproterenol on blood pressure and heart rate? |
|
Definition
Isoproterenol decreases blood pressure and increases heart rate. |
|
|
Term
List two uses of phenylephrine. |
|
Definition
Nasal decongestant and hypotension. |
|
|
Term
What is the receptor that phenylephrine binds to? |
|
Definition
|
|
Term
What is a side effect of phenylephrine? |
|
Definition
|
|
Term
What is methoxamine used for? |
|
Definition
Hypotension, pressor agent (not commonly used). |
|
|
Term
What receptor does methoxamine bind to? |
|
Definition
|
|
Term
What is a side effect of methoxamine? |
|
Definition
|
|
Term
What is clonidine used for? |
|
Definition
|
|
Term
What receptor does clonidine bind to, and is it an agonist or an antagonist? |
|
Definition
|
|
Term
What is the mechanism of clonidine action? |
|
Definition
It is an alpha-2 agonist that decreases CNS sympathetic outflow and inhibits the release of norepinephrine. |
|
|
Term
What is a major risk in discontinuing clonidine use? |
|
Definition
|
|
Term
What are three side effects of clonidine? |
|
Definition
Dry mouth, sedation, impotence. |
|
|
Term
What is alpha-methyldopa used for? |
|
Definition
|
|
Term
What is the mechanism of action of alpha-methyldopa? |
|
Definition
It binds to alpha-2 receptors and decreases CNS sympathetic output and norepinephrine release. |
|
|
Term
What is a risk of discontinuing alpha-methyldopa use? |
|
Definition
|
|
Term
List 3 side effects of alpha-methyldopa. |
|
Definition
Dry mouth, sedation, impotence. |
|
|
Term
What is alpha-methyldopa metabolized to? |
|
Definition
Alpha-methylnorepinephrine. |
|
|
Term
What are two uses of dobutamine? |
|
Definition
Congestive heart failure and cardiac stimulant. |
|
|
Term
What is the mechanism of dobutamine? |
|
Definition
It is a beta-1 agonist that increases force of contraction without increasing heart rate or oxygen demand. |
|
|
Term
List two problems with dobutamine. |
|
Definition
Tolerance and desensitization. |
|
|
Term
What is albuterol used for? |
|
Definition
|
|
Term
What receptor is albuterol selective for? |
|
Definition
It is beta-2 selective (agonist). |
|
|
Term
What is the onset and duration if albuterol is administered orally? |
|
Definition
1-2 hours to onset and 4-6 hour duration. |
|
|
Term
What is the onset and duration of albuterol if administered by inhalation? |
|
Definition
5-10 minute onset and 3-4 hour duration. |
|
|
Term
What type of side effects can occur with albuterol use? |
|
Definition
Cardiovascular (less with inhalation). |
|
|
Term
What is ritodrine used for? |
|
Definition
|
|
Term
What is ritodrine's mechanism. |
|
Definition
|
|
Term
Explain how mydriasis occurs. |
|
Definition
Activation of alpha-1 receptors on the radial muscle causes pupil dilation. |
|
|
Term
Explain how miosis occurs. |
|
Definition
Activation of M2 and M3 receptors on the circular muscle by the parasympathetic nervous system causes contraction of the circular muscle and pupil constriction. |
|
|
Term
Explain how accommodation occurs. |
|
Definition
Activation of M3 receptors on the ciliary muscle causes contraction. |
|
|
Term
Explain the receptor involved and the response to sympathetic stimulation of the heart. |
|
Definition
Activation of the beta-1 receptor causes increased heart rate and force of contraction. |
|
|
Term
Explain how the parasympathetic nervous system acts on the heart. |
|
Definition
Activation of M2 receptors causes a decrease in heart rate. |
|
|
Term
Explain how the sympathetic nervous system acts on the vascular muscle. |
|
Definition
Activation of alpha-1 receptors causes constriction. Activation of beta-2 receptors causes relaxation. |
|
|
Term
Explain how the parasympathetic nervous system acts on vascular muscle. |
|
Definition
NO causes relaxation (M3 receptor involved). |
|
|
Term
Explain how the sympathetic nervous system acts on bronchial muscle. |
|
Definition
Activation of beta-2 receptors causes relaxation. |
|
|
Term
Explain how the parasympathetic nervous system acts on bronchial muscle. |
|
Definition
Activation of M receptors causes contraction. |
|
|
Term
Explain how the sympathetic nervous system acts on the GI tract. |
|
Definition
Activation of the alpha-1 and beta-2 receptors decreases motility. |
|
|
Term
Explain how the parasympathetic nervous system acts on the GI tract. |
|
Definition
Activation of M3 receptors causes increased motility. |
|
|
Term
Explain how the sympathetic nervous system acts on genitourinary muscle. |
|
Definition
Activation of beta-2 receptors causes relaxation. |
|
|
Term
Explain how the parasympathetic nervous system acts on genitourinary muscle. |
|
Definition
Activation of M3 receptors causes contraction. |
|
|
Term
Explain how the sympathetic nervous system acts on the uterus. |
|
Definition
Activation of beta-2 receptors causes relaxation. |
|
|
Term
Explain how the sympathetic nervous system acts on the pilomotor muscles. |
|
Definition
Activation of alpha receptors causes contraction. |
|
|
Term
Explain how the sympathetic nervous system acts on the sweat glands. |
|
Definition
Activation of M3 receptors causes increased secretion. |
|
|
Term
Explain how the sympathetic nervous system acts on the liver. |
|
Definition
Activation of beta-2 receptors causes release of glucose. |
|
|
Term
Explain how the sympathetic nervous system acts on the kidney. |
|
Definition
Activation of beta-1 receptors increases renin. |
|
|
Term
Explain how the sympathetic nervous system acts on fat cells. |
|
Definition
Activation of beta-3 receptors stimulates lipolysis. |
|
|
Term
What second messenger is produced upon activation of beta receptors and D1 and D5 receptors? |
|
Definition
|
|
Term
What second messenger is produced upon activation of alpha-1 receptors and M1, M3, and M5 receptors? |
|
Definition
|
|
Term
What second messenger is affected by stimulation of alpha-2, M2, M4, D2,D3, and D4 receptors? |
|
Definition
|
|
Term
What ion flow occurs as a result of activation of nicotinic receptors? |
|
Definition
Sodium in, potassium out. |
|
|
Term
What is the formula for blood pressure? |
|
Definition
|
|
Term
What is the formula for cardiac output? |
|
Definition
|
|
Term
What does the baroreceptor reflex respond to? |
|
Definition
Blood pressure change (not heart rate change). |
|
|
Term
What is the effect of alpha-1 receptor activation on total peripheral resistance and blood pressure? |
|
Definition
Increased TPR, increased BP. |
|
|
Term
What is the effect of beta-1 receptor activation on heart rate, cardiac output, and blood pressure? |
|
Definition
|
|
Term
What is the effect of beta-2 receptor activation on total peripheral resistance and blood pressure? |
|
Definition
|
|
Term
What is the effect of M2 receptor activation on heart rate, cardiac output, and blood pressure? |
|
Definition
|
|
Term
What is the effect of M3 receptor activation on total peripheral resistance and blood pressure? |
|
Definition
|
|
Term
Are vascular beta-2 and M3 receptors innervated? |
|
Definition
|
|
Term
What is the effect of norepinephrine on heart rate and blood pressure? |
|
Definition
Decreased heart rate and increased blood pressure. |
|
|
Term
What is the effect of isoproterenol on blood pressure, heart rate, and PP? |
|
Definition
BP (o/-), increased heart rate, increased PP. |
|
|
Term
What is the effect of epinephrine on BP, HR, and PP? |
|
Definition
|
|
Term
What is the effect of mecamylamine on blood pressure and heart rate? |
|
Definition
Decreased blood pressure and (0/+) HR. |
|
|
Term
What is the effect of propranolol on blood pressure and heart rate? |
|
Definition
BP (0/-), decreased heart rate. |
|
|
Term
What is the effect of atropine on blood pressure and heart rate? |
|
Definition
BP (0/-), increased heart rate. |
|
|
Term
What is the effect of phentolamine on blood pressure, heart rate, and PP? |
|
Definition
Decreased blood pressure, increased heart rate, increased PP. |
|
|
Term
Epinephrine counters the effects of the physiological release of what molecule? |
|
Definition
|
|
Term
What is the effect of norepinephrine on renal vasculature? |
|
Definition
|
|
Term
What is the effect of dopamine on renal vasculature? |
|
Definition
|
|
Term
List two drugs of choice/frontline agents for chronic glaucoma. |
|
Definition
|
|
Term
What is the mechanism of action of timolol? |
|
Definition
It is a beta-blocker that helps glaucoma by decreasing secretion. |
|
|
Term
What is the mechanism of action of latanoprost? |
|
Definition
Latanoprost is a PGF2alpha analogue that treats chronic glaucoma by increasing outflow. |
|
|
Term
What are 3 side effects of latanoprost? |
|
Definition
Red eye, long eyelashes, and dark pupils. |
|
|
Term
List four frontline agents for hypertensive crisis. |
|
Definition
Alpha-blockers, labetalol, carvedilol, and fenoldopam. |
|
|
Term
What is the mechanism of action of labetalol and carvedilol? |
|
Definition
Alpha/beta blockers reduce blood pressure and heart rate. |
|
|
Term
Give two examples of alpha-blockers. |
|
Definition
Phenoxybenzamine and phentolamine. |
|
|
Term
What is the mechanism of action of Fenoldopam? |
|
Definition
D1a-agonist used for acute hypertension and renal failure. |
|
|
Term
Which beta-blockers are beta-1 selective? |
|
Definition
|
|
Term
List three contraindications for use of beta-blockers. |
|
Definition
Unstable CHF, asthma, and diabetes. |
|
|
Term
What is the front-line agent for emergency glaucoma treatment? |
|
Definition
|
|
Term
What is the mechanism of action of pilocarpine? |
|
Definition
M-agonist increases outflow. |
|
|
Term
What is the front-line agent for reversing atropine toxicity? |
|
Definition
|
|
Term
What is the mechanism of action of physostigmine? |
|
Definition
It is a reversible acetylcholinesterase inhibitor that can cross the BBB. |
|
|
Term
What is the front-line agent for regenerating acetylcholinesterase? |
|
Definition
|
|
Term
What is atropine a front-line agent for? |
|
Definition
Reversing acetylcholinesterase inhibition. |
|
|
Term
What is the front-line agent for malignant hyperthermia? |
|
Definition
|
|
Term
What is the mechanism of action of Dantrolene? |
|
Definition
It inhibits calcium release from the SR. |
|
|
Term
What is the cause of Raynaud's syndrome? |
|
Definition
Excessive sympathetic tone in nerves supplying the hands and feet. |
|
|
Term
What is the treatment for Raynaud's Syndrome? |
|
Definition
|
|
Term
What is the main way that norepinephrine signaling is terminated? |
|
Definition
Neuronal uptake (70-80%). |
|
|
Term
What is the mechanism of action of cocaine and tricyclic antidepressants? |
|
Definition
They inhibit the reuptake of norepinephrine. |
|
|
Term
What enzyme metabolizes re-uptooken norepinephrine in the neuron? |
|
Definition
|
|
Term
What enzyme metabolizes norepinephrine after extra-neuronal uptake? |
|
Definition
|
|
Term
Where in the cell is MAO? |
|
Definition
Mitochondrial outer membrane. |
|
|
Term
Where in the cell is COMT? |
|
Definition
|
|
Term
What MAO isoform is in the sympathetic nerves and placenta? |
|
Definition
|
|
Term
What MAO isoform is in the platelets? |
|
Definition
|
|
Term
What MAO isoform is in the liver, kidney, and brain? |
|
Definition
|
|
Term
List 2 effects of MAO inhibition. |
|
Definition
Increased norepinephrine level in sympathetic neuron. Potentiated release by tyramine-like drugs. |
|
|
Term
|
Definition
|
|
Term
What is tranylcypromine, and what is it used for? |
|
Definition
Tranylcypromine is a non-selective MAO inhibitor used for depression. |
|
|
Term
What is Selegiline, and what is it used for? |
|
Definition
Selegiline is a MAO-B inhibitor used for Parkinson's Disease. |
|
|
Term
|
Definition
Major metabolites of catecholamine metabolism. |
|
|
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the alpha-1 receptor. |
|
Definition
|
|
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the alpha-2 receptor. |
|
Definition
|
|
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-1 receptor. |
|
Definition
|
|
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-2 receptor. |
|
Definition
|
|
Term
List the relative affinities of epinephrine, norepinephrine, and isoproterenol for the beta-3 receptor. |
|
Definition
|
|
Term
Does norepinephrine cross the blood brain barrier? |
|
Definition
|
|
Term
Does epinephrine cross the blood brain barrier? |
|
Definition
|
|
Term
What receptor does dopamine activate at low doses? |
|
Definition
|
|
Term
What receptor does dopamine activate at moderate doses? |
|
Definition
|
|
Term
What receptor does dopamine activate at high doses? |
|
Definition
|
|
Term
|
Definition
Salmeterol is a LABA. It is a long-acting beta-2 agonist used for treatment of asthma and COPD. |
|
|
Term
What is Terbutaline, and what is it used for? |
|
Definition
Terbutaline is a beta-2 selective agonist used for asthma and premature labor. |
|
|
Term
What is dexmedetomidine, and what is it used for? |
|
Definition
It is an alpha-2 agonist that has CNS action and is used for sedation/analgesia in surgery. |
|
|
Term
What is a cause for caution in Dexmedetomidine use? |
|
Definition
|
|
Term
What is Tizanidine, and what is it used for? |
|
Definition
Tizanidine is an alpha-2 agonist used to treat muscle spasticity and multiple sclerosis. |
|
|
Term
What is a contraindication for Tizanidine use? |
|
Definition
|
|
Term
|
Definition
A dopamine agonist used to treat Parkinson's Disease and restless leg syndrome. |
|
|
Term
What is the first treatment that is typically used for Parkinson's Disease? |
|
Definition
|
|
Term
What is the purpose of carbidopa? |
|
Definition
It is a decarboxylase inhibitor that cannot cross the blood brain barrier. It prevents L-dopa from being converted into dopamine until it reaches the CNS. |
|
|
Term
What is Benztropine, and what is it used for? |
|
Definition
It is a cholinoceptor antagonist that is used for Parkinson's disease. |
|
|
Term
What are amphetamines used for, and what is their mechanism of action? |
|
Definition
Amphetamines are used for narcolepsy, ADHD, and appetite suppression. They work by displacing norepinephrine. |
|
|
Term
What class of drugs is methylpenidate in? |
|
Definition
Methylpenidate is an amphetamine. |
|
|
Term
What is the use of Ephedrine, and what is its mechanism of action? |
|
Definition
Ephedrine is used as a nasal decongestant. It has direct action on alpha and beta receptors and indirect action to release norepinephrine. |
|
|
Term
What types of drugs does Ephedrine interact with? |
|
Definition
|
|
Term
What is the mechanism of action of tyramine? |
|
Definition
It displaces neurotransmitter. |
|
|
Term
What does tyramine interact with? |
|
Definition
|
|
Term
What is a side effect of using MAOI and consuming foods high in tyramine? |
|
Definition
|
|
Term
Briefly define tachyphylaxis. |
|
Definition
Tachyphylaxis is a short-term decrease in response to a drug due to local depletion of neurotransmitter. |
|
|
Term
What class of drugs is susceptible to tachyphylaxis? |
|
Definition
|
|
Term
List the four effects involved in the mechanism of action of amphetamine and amphetamine-like stimulants. |
|
Definition
1. Binding to extracellular catecholamine receptors. 2. Inhibition of monoamine neurotransmitter uptake. 3. Release of catecholamines from neurons. 4. Inhibition of monoamine oxidase. |
|
|
Term
What is the mechanism of action of cocaine? |
|
Definition
It inhibits neuronal uptake. |
|
|
Term
What is the mechanism of action of tricyclic antidepressants? |
|
Definition
They inhibit neuronal uptake. |
|
|
Term
What is Imipramine, and how does it work? |
|
Definition
Imipramine is a tricyclic antidepressant that works by blocking neuronal uptake of norepinephrine. |
|
|
Term
What is Amitriptylline, and how does it work? |
|
Definition
Amitriptylline is a tricyclic antidepressant that works by blocking neuronal uptake. |
|
|
Term
List three side effects of tricyclic antidepressants. |
|
Definition
Dry mouth, blurred vision, decreased urination. |
|
|
Term
What are 3 toxic effects of high doses of tricyclic antidepressants? |
|
Definition
Severe anticholinergic effect, respiratory depression, and PHT (alpha-block) |
|
|
Term
What is Atomoxetine, and what is it used for? |
|
Definition
Atomoxetine is a tricyclic antidepressant used for ADHD. |
|
|
Term
What receptors do tricyclic antidepressants block at high doses? |
|
Definition
|
|
Term
What is a clinical use of COMT inhibitors? |
|
Definition
|
|
Term
How do MAO inhibitors potentiate the effects of tyramine? |
|
Definition
They block metabolism of tyramine by MAO in the liver. |
|
|
Term
What is the result of tyramine interactions with MAO inhibitors? |
|
Definition
Hypertensive crisis (increased blood pressure and heart rate). |
|
|
Term
What is the treatment for a tyramine crisis? |
|
Definition
Alpha-blockers or Labetalol (alpha, beta blocker). |
|
|
Term
State an appropriate drug to use for acute congestive heart failure. |
|
Definition
|
|
Term
State two sympathomimetics appropriate to use for cardiac heart block and cardiac arrest. |
|
Definition
Epinephrine and isoproterenol. |
|
|
Term
State an ophthalmic use of phenylephrine. |
|
Definition
|
|
Term
State an ophthalmic use of epinephrine. |
|
Definition
|
|
Term
What is the effect of bella-donna agents on pupil size? |
|
Definition
|
|
Term
|
Definition
An antagonist is a drug that has high affinity but no (or low) intrinsic activity. |
|
|
Term
Is phenoxybenzamine a reversible or irreversible alpha-1 antagonist? |
|
Definition
|
|
Term
Is phentolamine a reversible or irreversible alpha-1 antagonist? |
|
Definition
|
|
Term
List two drugs used to treat a hypertensive crisis caused by pheochromocytoma. |
|
Definition
Phenoxybenzamine and phentolamine. |
|
|
Term
What is the treatment for benign prostate hypertrophy? |
|
Definition
|
|
Term
What is the mechanism of action of prazosin? |
|
Definition
Alpha-1 receptor blocker. |
|
|
Term
What are two side-effects of phenoxybenzamine? |
|
Definition
Orthostatic hypotension and reflex tachycardia. |
|
|
Term
Describe the selectivity of phentolamine. |
|
Definition
Equally selective for alpha-1 and alpha-2 receptors. |
|
|
Term
What is the effect of beta blockers on total peripheral resistance and cardiac output? |
|
Definition
Gradual decrease in TPR despite long-term decrease in CO. |
|
|
Term
List four ways that beta-blockers are effective for hypertension treatment. |
|
Definition
CNS action to reduce sympathetic tone. Block of cardiac beta receptors. Block of presynaptic beta receptors to decrease NE release. Decrease in renin release. |
|
|
Term
What type of drug is commonly used for angina? |
|
Definition
|
|
Term
What type of drug is often used for arrhythmia? |
|
Definition
Beta-1 selective antagonists. |
|
|
Term
What type of drug can be used to treat tremor of peripheral origin? |
|
Definition
|
|
Term
What type of drug can be used for migraine prophylaxis? |
|
Definition
|
|
Term
What drug is used in hyperthyroidism to decrease cardiac manifestation? |
|
Definition
|
|
Term
What type of drug is used to treat panic attacks and stage fright? |
|
Definition
|
|
Term
Which beta-blocker is not used to treat hypertension? |
|
Definition
Esmolol (it is too short-acting). |
|
|
Term
List two uses of carvedilol. |
|
Definition
Hypertension and heart failure. |
|
|
Term
What is unique about the specificity of carvedilol and labetalol? |
|
Definition
They have alpha and beta-blocking activity. |
|
|
Term
List two uses of labetalol. |
|
Definition
|
|
Term
List two uses of pindolol. |
|
Definition
|
|
Term
List four uses of propranolol. |
|
Definition
Hypertension, angina, arrhythmia, and myocardial infarction (never for heart failure). |
|
|
Term
In addition to glaucoma, what are four other conditions that timolol can treat? |
|
Definition
Hypertension, angina, arrhythmia, and myocardial infarction. |
|
|
Term
What are four uses of atenolol? |
|
Definition
Hypertension, angina, arrhythmia, and myocardial infarction. |
|
|
Term
What is a contraindication for using atenolol? |
|
Definition
|
|
Term
What is esmolol used for? |
|
Definition
Operative arrhythmia (short-acting). |
|
|
Term
What are five uses of metoprolol? |
|
Definition
Hypertension, angina, arrhythmia, myocardial infarction, and heart failure. |
|
|
Term
What is nebivolol used for? |
|
Definition
It acts as a vasodilator (via NO) and is used for hypertension. |
|
|
Term
What is nebivolol selective for if less than 10 mg is used? |
|
Definition
|
|
Term
Which beta-blockers have less risk of rebound hypertension? |
|
Definition
Beta-blockers with partial agonist activity. |
|
|
Term
What type of beta-blocker should be used in patients with asthma? |
|
Definition
|
|
Term
What type of beta-blocker is preferred for patients with diabetes? |
|
Definition
Beta-1 selective, due to blocking of beta-2 receptors in the liver. |
|
|
Term
What is the effect of beta-blockers on Raynaud's disease? |
|
Definition
|
|
Term
What are three CNS side-effects of beta-blockers? |
|
Definition
Nightmares, depression, and insomnia. |
|
|
Term
How do the effectiveness and risk for adverse effects from beta-blockers in elderly patients compare with the effectiveness and risk of adverse effects in young patients? |
|
Definition
Beta-blockers are less effective and more risky for older patients. |
|
|
Term
What is haloperidol, and what is it used for? |
|
Definition
Haloperidol is a dopamine antagonist used for schizophrenia and nausea. |
|
|
Term
What are two side-effects of haloperidol? |
|
Definition
Tachycardia and hypo/hypertension. |
|
|
Term
What is the mechanism of action of hemicholinium? |
|
Definition
It inhibits choline uptake into the presynaptic neuron. |
|
|
Term
What is the mechanism of action of botulinum? |
|
Definition
It inhibits acetylcholine release. |
|
|
Term
What is the rate-limiting step of cholinergic neurotransmission? |
|
Definition
Uptake of choline into the nerve terminal. |
|
|
Term
What enzyme synthesizes acetylcholine? |
|
Definition
Choline acetyltransferase. |
|
|
Term
How is cholinergic neurotransmission terminated? |
|
Definition
|
|
Term
What type of acetylcholinesterase is at the nerves and neuromuscular junction? |
|
Definition
True acetylcholinesterase. |
|
|
Term
What type of acetylcholinesterase is in the circulation? |
|
Definition
|
|
Term
What receptors does acetylcholine act on? |
|
Definition
Muscarinic and nicotinic. |
|
|
Term
State two uses of bethanechol. |
|
Definition
Atonic gut and urinary retention. |
|
|
Term
What receptors does bethanechol act on? |
|
Definition
|
|
Term
What is methacholine used for? |
|
Definition
|
|
Term
What class of drugs does methacholine belong to? |
|
Definition
Cholinoceptor agonists (M agonist). |
|
|
Term
What class of drugs does carbachol belong to? |
|
Definition
Cholinoceptor agonist (M/some N). |
|
|
Term
What is carbachol used for? |
|
Definition
Glaucoma if pilocarpine is ineffective. |
|
|
Term
What is the mechanism of action of muscarine? |
|
Definition
Muscarinic receptor agonist. |
|
|
Term
What is the drug of choice for emergency glaucoma? |
|
Definition
|
|
Term
What class of drugs does pilocarpine belong to? |
|
Definition
|
|
Term
What muscarinic receptor agonist is diagnostic for belladonna poisoning? |
|
Definition
|
|
Term
List eight symptoms of muscarinic excess. |
|
Definition
Diarrhea Urination Miosis Bronchorrea (increased mucus) Bradycardia Emesis Lacrimation Salivation/sweating |
|
|
Term
List five symptoms of nicotinic excess. |
|
Definition
Mydriasis Tachycardia Weakness Hyperthermia Fasciculations |
|
|
Term
What class of drugs does nicotine belong to? |
|
Definition
Nicotinic receptor agonist. |
|
|
Term
What is varenicline used for? |
|
Definition
|
|
Term
What is the mechanism of action of varenicline? |
|
Definition
|
|
Term
Is physostigmine a reversible or irreversible acetylcholinesterase inhibitor? |
|
Definition
|
|
Term
Are organophosphates reversible or irreversible acetylcholinesterase inhibitors? |
|
Definition
|
|
Term
What drug is used to test for myasthenia gravis? |
|
Definition
|
|
Term
What class of drugs does edrophonium belong to? |
|
Definition
Reversible acetylcholinesterase inhibitors (quaternary ammonium compounds). |
|
|
Term
What class of drugs do physostigmine and neostigmine belong to? |
|
Definition
Reversible acetylcholinesterase inhibitors (carbamates). |
|
|
Term
Of physostigmine and neostigmine, which has CNS activity? |
|
Definition
|
|
Term
What drug is used to reverse atropine toxicity? |
|
Definition
|
|
Term
What are two uses of neostigmine? |
|
Definition
Reverse NMJ block and treat myasthenia gravis. |
|
|
Term
What is donepezil used for? |
|
Definition
Treatment of the symptoms of Alzheimer's disease. |
|
|
Term
What is the mechanism of action of donepezil? |
|
Definition
It is a reversible acetylcholinesterase inhibitor that has CNS activity. |
|
|
Term
|
Definition
|
|
Term
What is the mechanism of action of DFP? |
|
Definition
It is an irreversible acetylcholinesterase inhibitor. |
|
|
Term
What is echothiophate used for? |
|
Definition
|
|
Term
What is the mechanism of action of echothiophate? |
|
Definition
Irreversible acetylcholinesterase inhibitor. |
|
|
Term
Does echothiophate have CNS activity? |
|
Definition
|
|
Term
What is the mechanism of action of nerve gases? |
|
Definition
Irreversible acetylcholinesterase inhibitors. |
|
|
Term
What are malathion and parathion? |
|
Definition
Irreversible acetylcholinesterase inhibitors used in insecticides. |
|
|
Term
What is the purpose of 2-PAM? |
|
Definition
It can reverse the inhibition of acetylcholinesterase by organophosphates before aging has occurred. |
|
|
Term
Rank DFP, nerve gas, and insecticides from shortest to longest aging process. |
|
Definition
Nerve gas, DFP, insecticides. |
|
|
Term
What type of glaucoma can be treated with physostigmine and echothiophate? |
|
Definition
|
|
Term
What is the preferred drug to use for treatment of toxicity due to high concentrations of tricyclic antidepressants? |
|
Definition
|
|
Term
What is the mechanism of action of atropine? |
|
Definition
It blocks acetylcholine in parasympathetic effector junctions (muscarinic receptors). |
|
|
Term
What is the mechanism of action of trimethapan? |
|
Definition
It blocks acetylcholine in ganglia(both parasympathetic and sympathetic). |
|
|
Term
What is the mechanism of action of curare and succinylcholine? |
|
Definition
They block acetylcholine at the neuromuscular junction (skeletal muscle relaxants). |
|
|
Term
What is the effect of anticholinergic agents on the heart? |
|
Definition
Tachycardia and increased A-V nodal CV. |
|
|
Term
What is the effect of anticholinergic agents on the vasculature? |
|
Definition
No effect (vasodilation at toxic doses, though). |
|
|
Term
What is the effect of anticholinergic agents on the GI tract and urinary tract? |
|
Definition
Relaxation, decreased secretion, decreased motility. |
|
|
Term
What is the effect of anticholinergic agents on the lungs? |
|
Definition
Bronchial relaxation and decreased bronchial secretions. |
|
|
Term
What is the effect of anticholinergic agents on the eye? |
|
Definition
Mydriasis (sphincter relaxation) Cyclopegia (ciliary muscle relaxation) |
|
|
Term
What is the effect of anticholinergic agents on the CNS? |
|
Definition
Agitation, delirium, confusion. |
|
|
Term
What is scopolamine used for? |
|
Definition
|
|
Term
What is the mechanism of action of scopolamine? |
|
Definition
Antimuscarinic agent (like atropine). |
|
|
Term
What is ipratropium used for? |
|
Definition
|
|
Term
What is the mechanism of action of ipratropium? |
|
Definition
|
|
Term
What is tiotropium used for? |
|
Definition
|
|
Term
What is the mechanism of action of tiotropium? |
|
Definition
|
|
Term
What is benztropine used for? |
|
Definition
|
|
Term
What is the mechanism of action of benztropine? |
|
Definition
|
|
Term
What is propantheline used for? |
|
Definition
|
|
Term
What is the mechanism of action of propantheline? |
|
Definition
|
|
Term
List four clinical uses of botulinus toxin. |
|
Definition
Facial muscle spasms, strabismus, wrinkles, and migraine. |
|
|
Term
What is the treatment for atropine toxicity? |
|
Definition
Neostigmine or physostigmine. For hypotension, sympathomimetics (alpha agonist like methoxamine). |
|
|
Term
List six symptoms of antimuscarinic toxicity. |
|
Definition
Mad as a hatter: CNS, delirium. Red as a beet: Direct vasodilation. Blind as a bat: Cycloplegia. Hot as a hare: Decreased sweat, thermoregulation. Dry as a bone: Decreased secretion. At high concentrations, hypotension due to ganglionic block. |
|
|
Term
How do carbonic acid inhibitors treat glaucoma? |
|
Definition
|
|
Term
What is latanoprost used for? |
|
Definition
|
|
Term
How does latanoprost work? |
|
Definition
It is a prostaglandin analogue that treats glaucoma by increasing outflow. It also produces fuller lashes. |
|
|
Term
What is dorzolamide used for? |
|
Definition
|
|
Term
What is the mechanism of action of dorzolamide? |
|
Definition
It is a prostaglandin analogue that treats glaucoma by decreasing aqueous formation. |
|
|
Term
What glaucoma drug is contraindicated for patients with a sulfa drug allergy? |
|
Definition
|
|
Term
What is pyridostigmine used for? |
|
Definition
|
|
Term
What is the mechanism of action of pyridostigmine? |
|
Definition
Reversible acetylcholinesterase inhibition. |
|
|
Term
|
Definition
It is an oral ganglionic blocking agent used to decrease blood pressure during surgery. |
|
|
Term
|
Definition
The process of movement of a drug from its site of administration into plasma. |
|
|
Term
|
Definition
Movement of a drug from plasma into tissues and back. |
|
|
Term
What is the formula for the rate of diffusion of a drug across a lipid membrane? |
|
Definition
Rate of diffusion = -DAK(delta C)/Thickness. |
|
|
Term
What is the relationship between rate of filtration and drug concentration? |
|
Definition
Rate is directly proportional to drug concentration (1st order). |
|
|
Term
What is the equation for the half-life for drug absorption? |
|
Definition
|
|
Term
What is the formula for the amount of drug absorbed? |
|
Definition
|
|
Term
How can adverse systemic effects of local anesthetics be minimized? |
|
Definition
Use vasoconstrictors to reduce blood flow to the site of administration and reduce absorption into the plasma. |
|
|
Term
What is the main site of absorption for oral drugs? |
|
Definition
|
|
Term
What is the formula for bioavailability of a drug taken orally? |
|
Definition
F = AUC oral/AUC injected x 100 |
|
|
Term
What does metoclopramide do? |
|
Definition
It enhances gastric emptying rate. |
|
|
Term
What is the pharmacokinetic effect of antacids? |
|
Definition
Antacids affect the absorption of drugs requiring gastric fluid acidity for dissolution and form unabsorbable complexes with drugs in the gastrointestinal tract. |
|
|
Term
What is the pharmacokinetic effect of proton pump inhibitors? |
|
Definition
Proton pump inhibitors affect the absorption of drugs requiring gastric fluid acidity for dissolution. |
|
|
Term
What is the pharmacokinetic effect of cholestyramine? |
|
Definition
Cholestyramine affects absorption by adsorbing drugs in the gastrointestinal tract. |
|
|
Term
What is the pharmacokinetic effect of iron? |
|
Definition
Iron forms unabsorbable complexes with drugs in the gastrointestinal tract. |
|
|
Term
Where are fenestrated capillary beds located? |
|
Definition
Most tissues, including the kidney. |
|
|
Term
What types of drugs can pass through fenestrated capillary beds? |
|
Definition
Unbound drugs that do not have a large molecular weight. |
|
|
Term
Where are sinusoidal capillary beds located? |
|
Definition
|
|
Term
List three locations of closed capillary beds. |
|
Definition
|
|
Term
How can drugs pass through continuous (closed) capillary beds? |
|
Definition
Only by lipid diffusion or carrier-mediated transport. |
|
|
Term
What is thiopental used for? |
|
Definition
It is used as a sedative/hypnotic. |
|
|
Term
Why is thiopental an effective inducer of anesthesia? |
|
Definition
It distributes rapidly to the brain because it is a highly perfused tissue. |
|
|
Term
Why do the effects of thiopental terminate in 15-20 minutes? |
|
Definition
Slower but more effective distribution of the drug to non-target tissues with slower perfusion (fat and lean tissues). |
|
|
Term
How does the stomach function as a drug reservoir? |
|
Definition
The low pH traps basic drugs. |
|
|
Term
How does the liver function as a drug reservoir? |
|
Definition
The liver avidly binds drugs (chloroquine) |
|
|
Term
How do the bones and teeth act as drug reservoirs? |
|
Definition
They bind tetracyclines and fluoroquinolones (antibacterial drugs). |
|
|
Term
How does fat function as a drug reservoir? |
|
Definition
Fat concentrates lipid soluble drugs like thiopental. |
|
|
Term
What is the formula for volume of distribution? |
|
Definition
Vd = amount of drug in the body/C |
|
|
Term
What is the loading dose equation? |
|
Definition
|
|
Term
What is the equation for first-order rate of elimination? |
|
Definition
Rate of elimination = CL x C |
|
|
Term
What is the equation for the rate of zero-order elimination? |
|
Definition
|
|
Term
What is the equation for clearance? |
|
Definition
CL = rate of elimination/C |
|
|
Term
What is the equation for Kel in terms of Vd and CL? |
|
Definition
|
|
Term
What ise equation for half-life in terms of CL and Vd. |
|
Definition
|
|
Term
What type of elimination kinetics is followed by ethanol and phenytoin? |
|
Definition
|
|
Term
What are the three mechanisms that determine CLr? |
|
Definition
Glomerular filtration. Tubular secretion. Tubular reabsorption. |
|
|
Term
What is the equation for CL GF? |
|
Definition
CL GF = (Fraction of drug unbound in plasma)(GFR) |
|
|
Term
What is the glomerular filtration rate in a healthy adult? |
|
Definition
|
|
Term
What process is used to transport weak acids and weak bases on the blood-facing side in the kidney? |
|
Definition
|
|
Term
What process is used to transport drugs into the lumen of the nephron during secretion? |
|
Definition
Active transport by multidrug resistance proteins. |
|
|
Term
What is the maximum value of CL TS? |
|
Definition
|
|
Term
What must be true if CLr > CL GF? |
|
Definition
Secretion plays a role in elimination. |
|
|
Term
What is used to estimate RPF? |
|
Definition
Para-aminohippuric acid clearance. |
|
|
Term
What is the primary method of elimination for penicillin? |
|
Definition
Tubular secretion by OATs. |
|
|
Term
What is the effect of probenecid on tubular secretion? |
|
Definition
Probenecid is a weak acid that competes with weak acid drugs (like penicillin) for OATs. |
|
|
Term
What is the effect of cimetidine on tubular secretion? |
|
Definition
Cimetidine is a weak base that competes with other weak base drugs for OBTs. |
|
|
Term
State a clinical use of sodium bicarbonate. |
|
Definition
Sodium bicarbonate is used to alkalinize urine and increase excretion of weak acid drugs by decreasing reabsorption. |
|
|
Term
State a clinical use of ammonium chloride. |
|
Definition
Ammounium chloride is used to acidify the urine and increase the excretion of weak base drugs by decreasing reabsorption. |
|
|
Term
What are the cardiovascular effects of a high dose of phenylephrine? |
|
Definition
Increased blood pressure due to activation of alpha-1 receptors and vasoconstriction. Decreased heart rate due to reflex. |
|
|
Term
What are the cardiovascular effects of epinephrine? |
|
Definition
Increased blood pressure due to activation of alpha-1 receptors and beta-1 receptors. Increased heart rate due to activation of beta-1 receptors (attenuated by reflex bradycardia). |
|
|
Term
What are the cardiovascular effects of a high dose of isoproterenol? |
|
Definition
Decreased blood pressure due to activation of beta-2 receptors. Increased heart rate due to activation of beta-1 receptors + reflex. |
|
|
Term
What are the cardiovascular effects of epinephrine after phentolamine? |
|
Definition
Increased PP, decreased BP, increased HR (reflex). |
|
|
Term
Draw the diagram of the cardiovascular effects of a high dose of norepinephrine. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of a high dose of phenylephrine. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of a high dose of epinephrine. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of a high dose of isoproterenol. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of a high dose of phentolamine (an alpha-blocker). |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of a high dose of propranolol (a beta-blocker). |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + atropine. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + an alpha-blocker. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of norepinephrine + a beta-blocker. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of phenylephrine + atropine. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of epinephrine + an alpha-blocker. |
|
Definition
|
|
Term
Draw a diagram showing the cardiovascular effects of epinephrine + a beta-blocker. |
|
Definition
|
|
Term
What do Phase 1 enzymes do? |
|
Definition
Add or unmask functional group on a drug. |
|
|
Term
What do Phase 2 enzymes do? |
|
Definition
Phase 2 enzymes are conjugation enzymes that add an endogenous substance to the functional group to change the excretability or activity of a drug. |
|
|
Term
Where are cytochrome P450s and glucuronosyltransferases located in the cell? |
|
Definition
Smooth endoplasmic reticulum. |
|
|
Term
What is the pharmacokinetic effect of phenobarbital? |
|
Definition
Phenobarbital induces CYPs 2C9, 2C19, and 3A4. |
|
|
Term
What is the pharmacokinetic effect of rifampin? |
|
Definition
Inducer of CYPs 2C9, 2C19, 3A4 |
|
|
Term
What is the pharmacokinetic effect of phenytoin? |
|
Definition
Inducer of CYPs 2C9, 2C19, 3A4 , example of saturable kinetics of elimination |
|
|
Term
What is the pharmacokinetic effect of carbamazepine? |
|
Definition
Inducer of CYPs 2C9, 2C19, 3A4 |
|
|
Term
What is the pharmacokinetic effect of cigarette smoke? |
|
Definition
|
|
Term
What is the pharmacokinetic effect of alcohol? |
|
Definition
|
|
Term
What is the pharmacokinetic effect of St. John's wort? |
|
Definition
Inducer of CYPs 2C9, 2C19, 3A4 |
|
|
Term
What is the effect of cimetidine on drug metabolism? |
|
Definition
Broad spectrum inhibitor of many cytochrome P450s. |
|
|
Term
What is the pharmacokinetic effect of azole antifungals? |
|
Definition
Inhibitors of CYP2C9 and CYP3A4 |
|
|
Term
What is the pharmacokinetic effect of macrolide antibacterials? |
|
Definition
|
|
Term
What is the pharmacokinetic effect of HIV protease inhibitors? |
|
Definition
|
|
Term
What is the pharmacokinetic effect of grapefruit juice? |
|
Definition
Inhibitor of CYP3A4 (intestinal form only). |
|
|
Term
What cytochrome metabolizes theophylline? |
|
Definition
|
|
Term
What cytochrome metabolizes warfarin? |
|
Definition
|
|
Term
What are the effects of cholestasis and choleresis on CLbiliary? |
|
Definition
Cholestasis decreases CLbiliary. Choleresis increases CLbiliary. |
|
|
Term
What is the approximate CLh of high hepatic extraction drugs? |
|
Definition
|
|
Term
Do inducers and inhibitors of drug metabolism have a high effect on high hepatic extraction drugs? |
|
Definition
|
|
Term
Is the CLh of low hepatic extraction drugs highly affected by inducers or inhibitors of drug metabolism? |
|
Definition
|
|
Term
What is the mechanism of carbon monoxide toxicity? |
|
Definition
It binds to iron in hemoglobin, myoglobin, and cytochrome oxidase. It binds to hemoglobin with a higher affinity than oxygen. |
|
|
Term
What is the effect of carbon monoxide on the hemoglobin saturation curve? |
|
Definition
|
|
Term
What is the effect of CO toxicity on blood pressure? |
|
Definition
Hypotension due to myocardial toxicity and peripheral vasodilation. |
|
|
Term
What is the effect of CO toxicity on blood pH? |
|
Definition
|
|
Term
What are the symptoms of amphetamine toxicity? |
|
Definition
Sympathomimetic toxidrome. |
|
|
Term
What class of drugs is used to treat amphetamine toxicity? |
|
Definition
|
|
Term
What toxicity is treated with midazolam, lorazepam and diazepam? |
|
Definition
|
|
Term
Which CYP enzyme system makes the toxic metabolite from acetaminophen? |
|
Definition
|
|
Term
What stage of acetaminophen toxicity is characterized by nausea, vomiting, epigastric pain, pallor, and diaphoresis? |
|
Definition
Stage 1 (30 minutes to 24 hours). |
|
|
Term
In what stage of acetaminophen toxicity do lab abnormalities and RUQ pain begin? |
|
Definition
|
|
Term
In what stage of acetaminophen toxicity do liver and kidney failure develop and lab abnormalities peak? |
|
Definition
Stage 3 (72 to 96 hours). |
|
|
Term
What stage of acetaminophen toxicity involves either death or resolution? |
|
Definition
|
|
Term
At 4 hours after acetaminophen ingestion, what acetaminophen level warrants treatment? |
|
Definition
150 micrograms per milliliter. |
|
|
Term
What is the treatment for acetaminophen toxicity? |
|
Definition
|
|
Term
What is the mechanism of action of NAC? |
|
Definition
NAC is converted to glutathione and converts NAPQI into nontoxic metabolites. |
|
|
Term
What is the mechanism of toxicity of aspirin? |
|
Definition
It uncouples oxidative phosphorylation. |
|
|
Term
What toxicity causes high anion gap metabolic acidosis and respiratory alkalosis? |
|
Definition
|
|
Term
What toxicity causes tinnitus, hearing loss, hallucinations, agitation, coma, and seizures? |
|
Definition
|
|
Term
What is the treatment of aspirin toxicity? |
|
Definition
Sodium bicarbonate infusion. |
|
|
Term
What is the renal toxic metabolite of ethylene glycol? |
|
Definition
|
|
Term
How soon do you see evidence of renal failure after ethylene glycol poisoning? |
|
Definition
|
|
Term
What antidote was previously used to treat ethylene glycol poisoning? |
|
Definition
Ethanol (alcohol dehydrogenase inhibitor). |
|
|
Term
What is the treatment for ethylene glycol toxicity? |
|
Definition
|
|
Term
What is the mechanism of toxicity of lead? |
|
Definition
It binds to proteins and enzymes. |
|
|
Term
What toxicity is associated with a decrease in IQ? |
|
Definition
|
|
Term
What toxicity is associated with basophilic stippling? |
|
Definition
|
|
Term
What toxicity is associated with hypertension, chromosomal abnormalities, decreased testicular function, delayed menses, colicky pain, and constipation? |
|
Definition
|
|
Term
What is the most effective method to treat chronic lead exposure? |
|
Definition
|
|
Term
What is the toxic metabolite of methanol? |
|
Definition
Formaldehyde and formic acid. |
|
|
Term
What toxicity is associated with visual symptoms, such as snow storm vision, within 24 hours? |
|
Definition
|
|
Term
What is the mechanism of toxicity of cyanide? |
|
Definition
It binds to cytochrome oxidase and inhibits ATP production. It also decreases the use of oxygen, resulting in bright red venous blood. |
|
|
Term
What is the treatment for methanol poisoning? |
|
Definition
|
|
Term
What is the pharmacological treatment for lead poisoning? |
|
Definition
|
|
Term
What is the major symptom of CO poisoning? |
|
Definition
|
|
Term
What is the treatment for CO poisoning? |
|
Definition
|
|
Term
What is the major symptom of CN poisoning? |
|
Definition
|
|
Term
What is the treatment for CN poisoning? |
|
Definition
|
|
Term
Does tubocurarine cause histamine release? |
|
Definition
|
|
Term
Does tubocurarine block ganglionic receptors? |
|
Definition
Yes, at high concentrations. |
|
|
Term
How does the histamine release of pancuronium compare with the histamine release by tubocurarine? |
|
Definition
Less histamine is released by pancuronium. |
|
|
Term
Does pancuronium cause a ganglionic blockade? |
|
Definition
|
|
Term
What is important about the onset of rocuronium? |
|
Definition
Rocuronium has fast onset (1-2 minutes). |
|
|
Term
What is the advantage of cisatracurium? |
|
Definition
It is degraded by organ-independent Hoffmann degradation. |
|
|
Term
How is toxicity of competitive neuromuscular junction antagonists reversed? |
|
Definition
Acetylcholinesterase inhibitors such as neostigmine. |
|
|
Term
Does succinylcholine cause more or less histamine release and ganglionic blocking than tubocurarine? |
|
Definition
|
|
Term
Are the effects of succinylcholine reversed by acetylcholinesterase inhibitors? |
|
Definition
|
|
Term
What is the treatment for succinylcholine toxicity? |
|
Definition
|
|
Term
List three adverse effects of succinylcholine. |
|
Definition
Apnea in patients with atypical pseudo-acetylcholinesterase. Hyperkalemia, especially in burn and trauma patients, 2-7 hours after use. Malignant hyperthermia. |
|
|
Term
What drug increases the likelihood of malignant hyperthermia caused by succinylcholine? |
|
Definition
|
|
Term
What drug is used to treat malignant hyperthermia? |
|
Definition
|
|
Term
What is the mechanism of action of dantrolene? |
|
Definition
Decrease calcium release. |
|
|
Term
How do calcium channel blockers like verapamil interact with NMJ blocking agents? |
|
Definition
Decrease acetylcholine release. |
|
|
Term
How do aminoglycoside antibiotics interact with NMJ blockers? |
|
Definition
They compete with calcium to decrease acetylcholine release and stabilize the membrane. |
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How do certain general anesthetics such as halothane interact with NMJ blockers? |
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What is the steady state rate equation? |
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What can you conclude if EC50 |
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Less than 36 weeks gestation. |
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What is the formula for therapeutic index? |
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What is the equation for Certain Safety Factor? |
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Compare the elimination half-life of diazepam in neonates, infants, and adults. |
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Definition
The elimination half-life of diazepam is greatest in neonates and the elderly and shortest in infants/children. |
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List the steps of drug development and testing. |
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Definition
In vitro studies, animal testing, phase 1-3 clinical trials, postmarketing surveillance. |
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What is the goal of phase 1 clinical trials? |
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Definition
Establish limits of safe clinical dosage range. |
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What is done in phase 2 clinical trials? |
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Definition
The drug is tested in a small number of patients with the target disease to determine the efficacy, safety, and optimum dose. |
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What is done in phase 3 clinical trials? |
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Definition
The drug is studied in a large number of patients to further establish the safety and efficacy. |
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When is a New Drug Application filed? |
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Definition
After the clinical trials. |
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Term
Explain the important polymorphism of the beta-2 adrenergic receptor discussed in class. |
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Definition
Individuals with the G16 variant (60% of Hispanic/Caucasian individuals) down-regulate the beta-2 adrenergic receptor in response to agonists. Albuterol is less effective in G16 individuals. |
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As discussed in class, a polymorphism in what cytochrome P450 enzyme leads to unusual responses to phenytoin? |
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As discussed in class, a polymorphism in what cytochrome P450 enzyme affects the appropriate dose of warfarin? |
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What cytochrome P450 enzyme metabolizes codeine into morphine? |
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