Pharmacology I Exam 1: DRUGS Part III

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DRUGS For Exam 1 Part III

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Representative agents of agonists which act at BOTH alpha and beta receptors are:
Norepinephrine and Epinephrine
Both NE and E are full agonists at ALL adrenergic receptors but differ in:
Their affinities
NE is increased at:
Alpha-1, alpha-2, and beta-1
Epi is increased at:
Beta-1 and beta-2
NE and E are not given orally because:
They will be chewed up in the mucosa then metabolized by MAO and COMT
Cardiovascular effects: Large doses of NE produce:
Dramatic increase in TPR, HR, and BP
Cardiovascular effects: Large doses of E produce:
Similar effects to NE, except that TPR is less
Cardiovascular effects: Small doses of NE produce:
Increase in TPR and BP, but HR may decrease
Cardiovascular effects: Small doses of E produce:
Decrease TPR, Increase HR, and have little effect on BP
NE and E are used to produce:
Local vasoconstriction: in nose/throat/oral surgery, and with local anesthetics
NE and E are used to treat: (5)
Open-angle glaucoma, cardiovascular shock, cardiac arrest, bronchial asthma, anaphylactic shock
Cardiac adverse effects of NE and E are: (3)
Palpitations, anginal pain, cardiac arrhythmias
Other adverse effects of NE and E are: (4)
Cerebral hemorrhage, headache, tremor, anxiety
Alpha-1 receptor agonist representative agents include: (3)
Phenylephrine, Oxymetazoline, and Tetrahydrozoline
Phenylephrine is used for: (4)
As a mydriatic, treatment of cardiovascular shock, in combo with local anesthetics, to produce nasal and ocular decongestion
Oxymetazoline and Tetrahydrozoline are used for:
Mainly for nasal and ocular decongestion
Adverse effects for ALL alpha-1 agonists: (3)
Rebound nasal and ocular congestion, peripheral vasoconstriction, difficult urination
Contraindications for ALL alpha-1 agonists include: (6)
Diabetes, hypertension, heart disease, hyperthyroidism, narrow-angle glaucoma, prostatic hypertrophy
Alpha-2 receptor agonists include:
Clonidine and Methyldopa
Clonidine and Methyldopa are mainly used for:
Treatment of hypertension
Alpha-2 receptor agonist primary mechanism of antihypertensive action:
Stimulation of postsynaptic alpha-2 receptors in the CNS leading to a decrease in SNS activity
Alpha-2 receptor agonist secondary mechanism of antihypertensive action:
Stimulation of alpha-2 autoreceptors on ANS sympathetic nerve terminals leading to a decreased release of NE
Antihypertensive antagonistic effect:
Direct stimulation of postsynaptic alpha-2 receptors on blood vessels, leading to vasoconstriction
Clonidine is a:
Direct alpha-2 agonist
Methyldopa has:
NO direct alpha-2 agonistic activity (it is stored in synaptic vesicles as a "false neurotransmitter") and released by nerve action potential
Adverse effects of alpha-2 agonists: (2)
Sedation and dry mouth
Clonidine is actually useful to produce:
Agonists acting at BOTH beta-1 and beta-2 receptor representative agent is:
Isoproterenol pharmacological actions include: (2)
Increased rate and force of cardiac contraction, bronchodilation (beta-2 action)
I.V. beta receptor agonists are used as:
An emergency cardiostimulant
Inhaled beta receptor agonists are used as:
Bronchodilator in asthma
Adverse effects of beta receptor agonists are similar to:
Epinephrine, EXCEPT that no local necrosis, headache and cerebral hemorrhage
Agonists selective for beta-1 receptors include:
There are NO therapeutically useful agents that can be classified as beta-1 agonists
Beta-2 receptor agonist representative agents include:
Albuterol, Terbutaline, Salmeterol
Beta-2 receptor agonists have ________ selectivity for beta-2 versus beta-1:
Modest selectivity, increased doses produce beta-1 stimulation as well
Two important uses of beta-2 agonists are:
To produce bronchodilation in asthma and to produce uterine relaxation to prevent premature delivery
Albuterol and Terbutaline are used in these circumstances:
Rescue circumstances
Salmeterol can be used:
Everyday because of it's long half-life
Effects of beta-2 agonists: (3)
Bronchodilation, increased mucociliary clearance, decreased mast cell release of inflammatory mediators
Downregulation of beta-2 receptor agonists produces:
Tolerance for these agents
Ritodrine is given orally in order to:
Relax the uterus to prevent premature labor
The most common adverse effect of beta-2 agonists is:
Other adverse effects of beta-2 agonists include: (4)
Tachycardia, hypotension/dizziness, anxiety, hyperglycemia (because increased gluconeogenesis)
The FUNDAMENTAL mechanism of action of sympathomimetic amines is:
These drugs cause NE to be released from PREjunctional noradrenergic nerve terminals, this produces an effect
Representative agents for sympathomimetic amines include: (5)
Tyramine, Ephedrine, Pseudoephedrine, Amphetamine, Methamphetamine
Tyramine almost entirely acts:
Indirectly (by releasing NE)
Tyramine has NO:
Medical uses
Tyramine is present:
In large amounts in certain foods
Tyramine is a substrate for:
MAO, so little normally reaches the systemic circulation
MAO inhibition on Tyramine actions produces the accumulation of large amounts of NE in PREjunctional terminals, permitting:
Ingested Tyramine to reach systemic circulation in large amounts, large amounts of NE are released, can result in very large BP increase, can be fatal
All sympathomimetic amines with an indirect component of action are contraindicated in people taking:
MAO inhibitors
Ephedrine acts:
Mostly indirectly, but some direct action on beta-2 receptors
Ephedrine is mainly used for:
Bronchodilation in asthma
Ephedrine has significant CNS stimulation:
Probably due to release of both NE and DA, this can lead to abuse
Pseudoephedrine is a stereoisomer of:
Pseudoephedrine acts mainly:
Pseudoephedrine is mainly used for:
Nasal decongestion
Pseudoephedrine stimulation is:
Less than with Ephedrine
Amphetamine is an:
Indirectly acting sympathomimetic amine which has powerful CNS stimulating effects
Amphetamine is used for:
Appetite suppression, treatment of ADHD, treatment of narcolepsy
Most peripheral adverse effects of indirect acting sympathomimetic amines are those that would be produced by:
The combination of a non-specific alpha receptor agonist and a beta-1 receptor agonist
Other adverse effects of indirectly acting sympathomimetic amines include (6):
Hypertensive crisis (when taken w MAO inhibitors), insomnia, nervousness, irritability, mood elevation leading to abuse
Contraindications of sympathomimetic amines are similar to:
Direct acting alpha and beta receptor agonists, and also in people taking MAO inhibitors
Indirectly acting sympathomimetic amines don't produce much beta-2 effect except for:
Alpha receptor non-selective antagonist representative agent for haloalkylamines is:
Non-selective alpha receptor antagonists produce:
Competitive IRREVERSIBLE blockade of alpha-1 and alpha-2 receptors by forming a covalent bond with the receptor
Phenoxybenzamine is a very long lasting drug because:
The only way to get receptor function back is to synthesize new receptors, this can take days
Phenoxybenzamine's pharmacological actions include: (4)
Vasodilation, hypotension, tachycardia, "epinephrine reversal"
Phenoxybenzamine produces vasodilation and hypertension due to:
Block of alpha-1 and postjunctional alpha-2 receptors on arteries and veins
Phenoxybenzamine produces tachycardia through:
Baroreceptor reflex response, blockade of autoreceptors
Phenoxybenzamine produces effects that would be expected from:
Removal of sympathetic alpha receptor tone
Phenoxybenzamine is mainly used for:
Treatment of hypertension in tumors (not used very much anymore)
These adverse effects cause people to avoid Phenoxybenzamine:
Postural hypotension, tachycardia, cardiac arrhythmias
Other adverse effects of Phenoxybenzamine include: (4)
Nasal congestion, miosis, impaired ejaculation, diarrhea
Alpha receptor non-selective antagonist representative agent for imidazoollines is:
Phentolamine produces:
Competitive REVERSIBLE blockade of alpha-1 and alpha-2 receptors
Phentolamine pharmacological actions are similar to Phenoxybenzamine except:
They have a shorter duration of action
Phentolamine is used for: (2)
Treatment of Hypertensive episodes in tumors, treatment of impotence by intrapenile injection
Adverse effects of Phentolamine are:
Similar to Phenoxybenzamine but shorter-lasting
Alpha-1 receptor antagonist representative agent is:
Prazosin produces:
Highly selective competitive reversible blockade of alpha-1 receptors
Prazosin produces fewer ___________ than nonspecific alpha blockers:
Cardiac arrhythmias and less tachycardia, because don't block postsynaptic alpha-2 receptors so vasoconstriction still occurs
Prazosin is used for treatment of: (5)
Chronic hypertension, congestive heart failure, peripheral vascular disease, hemorrhagic shock, benign prostatic hypertrophy urinary problems
Adverse effects of Prazosin include:
"First dose phenomenon" (big drop in BP with first dose), chronic postural hypotension
Tamsulosin is an:
Alpha-1 receptor antagonist with selectivity for alpha-1a receptors, also called Flomax
Tamsulosin (Flomax) treats:
Benign prostatic hypertrophy, allows pt to pee
Alpha-2 receptor selective antagonist representative agent is:
Yohimbine produces:
Competitive reversible antagonism of alpha-2 receptors
Pharmacological actions of Yohimbine include: (3)
Enhanced sympathetic outflow, enhanced NE release, vasodilation
While Yohimbine has NO documented therapeutic usefulness, it may be effective in:
Treatment of psychogenic impotence, postural hypotension
Non-selective beta receptor antagonists (beta-blocker) representative agent is:
Propanolol produces:
Competitive reversible blockade of beta-1 and beta-2 receptors
Pharmacological actions of Propranolol in the heart include decreased:
Heart rate, force of contraction, cardiac output and automaticity
Pharmacological actions of Propranolol in the kidney include inhibition of:
Renin release resulting in a decrease in circulating levels of angiotensin II and aldosterone
Pharmacological actions of Propranolol in the lung include:
Slight bronchoconstriction in normals but can produce a dramatic bronchoconstriction in person with asthma or COPD
Metabolic effects of Propranolol include: (2)
Little effect on insulin release, inhibition of lipolysis
In insulin-dependent diabetics, an adverse effect of Propranolol is that it may:
Delay recovery from hypoglycemia, increase exercise-induced hypoglycemia, bc beta-blockers block beta-2 induced gluconeogenesis involved in recovery
Chronic use of Propranolol may:
Increase VLDL (bad cholesterol) and decrease HDL (good cholesterol)
Other effects of Propranolol include: (3)
Reduction of intraocular pressure, reduction of chatecholamine-induced tremor, local anesthetic activity
In the heart, beta-blockers like Propranolol are used to treat: (4)
Cardiac dysrhythmias, congestive heart failure, cardioprotection after heart attack, angina pectoris
Beta blockers like Propranolol are also used to treat: (6)
Hypertension, hyperthyroidism, open-angle glaucoma, prevention of migraine, anxiety, tremor
Adverse effects of beta blockers like Propranolol in the heart include:
Heart failure, cardiac dysrhythmia
Other adverse effects of beta blockers like Propranolol include: (6)
Bronchospasm, cold extremities (very common), fatigue, psychic depression, insomnia, nightmares
In diabetics, an adverse effect of Propranolol is that it may mask:
Tachycardia as a sign of hypoglycemia
Adverse rebound (withdrawal) effects of beta blockers like Propranolol include:
BP, HR, force of contraction and automaticity may all rise to excessive levels following abrupt withdrawal
Beta-1 receptor selective antagonist representative agent is:
Atenolol produces:
Competitive reversible blockade of beta receptors
Atenolol has a ________ selectivity for beta-1 versus beta-2 receptors:
Only a modest selectivity
Atenolol's pharmacological uses are similar to non-selective beta blockers, except that:
Atenolol is preferred for patients with bronchospasm, diabetes or peripheral vascular disease
Pharmacological actions and adverse effects of Atenolol are:
Similar to those produced by non-selective beta blockers but with a lesser tendency toward beta-2 mediated effects
Pindolol is both:
Beta receptor antagonist and partial agonist
Antagonists which act at BOTH alpha and beta receptors representative agents are:
Labetalol and Carvedilol
Labetalol and Carvedilol are mixtures of:
Stereoisomers in which the individual components have varying activity as antagonists at beta-1, beta-2, and alpha-1 receptors
Labetalol and Carvedilol produce NO:
Alpha-2 receptor blockade
Labetalol and Carvedilol's effects and adverse effects are:
Similar to the combined use of an alpha-1 receptor antagonist and non-selective beta antagonist
Labetalol and Carvedilol are used for: (4)
Acute hypertensive emergencies, essential hypertension, congestive heart failure, left ventricular failure subsequent to heart attack
Ergot alkaloids pharmacological actions:
Some are partial agonists (alpha receptors), agonists, antagonists or all 3 at certain 5HT and DA receptors
Most Ergot alkaloids produce:
Contraction of smooth muscle as a key effect, especially that of vasculature and the uterus
Ergotamine is used for:
Symptomatic relief of migraine headache pain
Ergonovine/Ergometrine is used for:
Control of postpartum uterine bleeding
Adverse effects of Ergot alkaloids include:
Nausea, vomiting, uterine spasm, rebound headache, signs of peripheral vasoconstriction
Contraindications for Ergot alkaloids include:
Pregnancy, peripheral vascular disease, coronary artery disease, hypertension, impaired liver function
Reserpine causes:
Irreversible block of vesicular storage of neurotransmitters bc it depletes NE, 5HT and DA in the periphery and CNS
The autonomic effects of high doses of Reserpine are equivalent to:
A chemical sypathectomy
Small doses of Reserpine are useful in:
Treating chronic hypertension
Guanethidine inhibits the release of:
NE from sympathetic nerve terminals (NOT the adrenal gland), primarily by acting as a false neurotransmitter
Guanethidine's effect is:
Guanethidine's autonomic effects are similar to:
Guanethidine is useful in treating:
Chronic Hypertension