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56 Cards in this Set

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Bethanechol
Bethanechol (a chemical modification of ACh) is a direct acting Muscarinic receptor agonist and is completely resistant to AChE. It has a (NH2 and CH3 attached) protecting it from AChE and making it more selective for Muscarinic receptors.

It will cause Meiosis (contraction of pupil) and anterior chamber of eye to drain reducing pressure. It will decrease HR and contractility.

It will increase respiratory mucus secretions and bronchialconstriction. It will increase peristalsis (GI muscle activity) and GI secretions, and will decrease esophageal tone in patients with GERD.

It will stimulate the detrusor muscle and relax the bladder sphincter increasing bladder voiding.

Side-effects include: sweating, NVD, +salivation
Carbachol
Carbachol (a chemical modification of ACh) is a non-selective (Nicotinic/Muscarinic) receptor agonist. It is completely resistant to AChE. (It has a NH2 attached)
Methacholine
Methacholine (a chemical modification of ACh) is a direct acting Muscarinic receptor agonist (due to CH3)

It will cause Meiosis (contraction of pupil) and anterior chamber of eye to drain reducing pressure. It will decrease HR and contractility.

It will increase respiratory mucus secretions and bronchial-constriction. Methacholine challenge is used to diagnose asthma.

It will increase peristalsis (GI muscle activity) and GI secretions.

Side-effects include: sweating, NVD, +salivation
Pilocarpine
Pilocarpine is a natrual alkaloid and is a tertiary amine that directly activates Muscarinic receptors.

It is useful for inducing salivation for the treatment of dry-mouth due to Sjogren's Syndrome.

Toxicities could include: convulsions, respiratory paralysis, HTN, and cardio arrythmias.
Varenicline
Varenicline is a Nicotinic receptor agonist that has selectivity for neuronal receptors.

It stimulates nicotinic receptors in the CNS and indirectly stimulates the mesolimbic dopamine system in the CNS that is important for the reward system after smoking.

It is used as a smoking cessation treatment
Donepezil
Donepezil is a reversible & noncompetitive (non-classic) AChE inhibitor.

This drug is used to treat Alzheimer's and can cause NVD and possible hepatotoxicity.
Edrophonium
Edrophonium binds reversibly with the active site of AChE and competitively inhibits the breakdown of ACh.

This drug is useful at diagnosing myasthenia gravis, a autoimmune disease affecting postsynaptic nicotinic ACh receptors at the neuromuscular junction.

It can also be used to treat Alzheimer's disease be allowing more ACh to increase cholinergic neurotransmission.
Galantamine
Galantamine binds reversibly with the active site of AChE and competitively inhibits the breakdown of ACh.

It can also be used to treat Alzheimer's disease be allowing more ACh to increase cholinergic neurotransmission.
Neostigmine
Neostigmine is a slowly reversible noncompetitive AChE inhibitor.

This drug stimulates the detrusor muscle and relaxes the sphincter muscle in the bladder and is used to treat urinary retention.

It is also useful for the chronic treatment of myasthenia gravis.

Patients could experience NVD
Pyridostigmine
Pyridostigmine is a slowly reversible noncompetitive AChE inhibitor.

It is useful for the chronic treatment of myasthenia gravis.

Patients could experience NVD
Rivastigmine
Rivastigmine is a slowly reversible noncompetitive AChE inhibitor.

It is used in the treatment of Alzheimer's disease.

Patients could experience NVD
Tacrine
Tacrine is a reversible & noncompetitive (non-classic) AChE inhibitor.

This drug is used to treat Alzheimer's and can cause NVD and is known for its drug-induced hepatotoxicity.
Atropine
Atropine is a naturally occuring antimuscarinic drug that blocks the binding of ACh at muscarinic receptors.

It can cause cycloplegia and mydriasis (pupil dilation and unable to focus). It can also increase HR and is used to treat bradycardia/MI.

It increases bronchodilation and decreases secretions. It also decreases GI secretions and motility.

It decreases urinary voiding. And can cause sedation at low dose, delirium and hallucinations at high doses.

Common side-effects include: dry mouth, blurred vision, sweating, delirum, constipation, urinary retention.
Scopolamine
Scopolamine is a naturally occuring antimuscarinic drug that blocks the binding of ACh at muscarinic receptors.

It can cause cycloplegia and mydriasis (pupil dilation and unable to focus). It can also increase HR and is used to treat bradycardia/MI.

It increases bronchodilation and decreases secretions. It also decreases GI secretions and motility.

It decreases urinary voiding. And can cause sedation at low dose, delirium and hallucinations at high doses.

Common side-effects include: dry mouth, blurred vision, sweating, delirum, constipation, urinary retention.
Homatropine
Homatropine is a semisynthetic chemical similar to atropine that blocks the binding of ACh at muscarinic receptors.

It can cause cycloplegia and mydriasis (pupil dilation and unable to focus). It can also increase HR and is used to treat bradycardia/MI.

It increases bronchodilation and decreases secretions. It also decreases GI secretions and motility.

It decreases urinary voiding. And can cause sedation at low dose, delirium and hallucinations at high doses.

Common side-effects include: dry mouth, blurred vision, sweating, delirum, constipation, urinary retention.
Ipratropium
Ipratropium is a quaternary amine antimuscarinic drug that has a permanetly charged N+ atom that keeps it from penetrating the CNS.

It is mainly used for its bronchodilation abilities and its ability to decrease secretions for patients with COPD
Tiotropium
Tiotropium is a quaternary amine antimuscarinic drug that has a permanetly charged N+ atom that keeps it from penetrating the CNS.

It is mainly used for its bronchodilation abilities and its ability to decrease secretions for patients with COPD
Trospinum
Trospinum is a quaternary amine antimuscarinic drug that has a permanetly charged N+ atom that keeps it from penetrating the CNS.

It is mainly used to help patients control urinary release and allow them to gain urinary continence.
Benztropine
Benztropine is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.

It can be used to treat Parkinson's disease do to its ability to decrease ACh activity in the CNS
Darifenacin
Darifenacin is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.

It is mainly used to help patients control urinary release and allow them to gain urinary continence.

This drug is selective for M3 receptors and will have fewer side-effects.
Dicyclomine
Dicyclomine is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.
Oxybutynin
Oxybutynin is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.

It is mainly used to help patients control urinary release and allow them to gain urinary continence.
Solifenacin
Solifenacin is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.

It is mainly used to help patients control urinary release and allow them to gain urinary continence.
Tolterodine
Tolterodine is a tertiary amine antimuscarinic drug that is well absorbed through the CNS.

It is mainly used to help patients control urinary release and allow them to gain urinary continence.
Phenylephrine
Phenylephrine is a Alpha-1 Selective Adrenergic Agonist.

In the eye this drug causes Mydriasis (contraction of the pupillary dialator muscle) and it decreases intraocular pressure.

In the heart is can cause significant vasoconstriction and is used to treat life-threatening hypotension.

It will also cause vasoconstriction in the upper respiratory and treats congestion.

In the UT it contracts the sphincter and prostate leading to decreased urine output.
Oxymetazoline
Oxymetazoline is a Non-selective Alpha Agonist.

It is mainly used to treat nasal congestion by causing vasoconstriction in the upper respiratory.

Pateints may build up a tolerance after prolonged use and might experience rebound nasal congestion after discontinuing the drug.
Naphazoline
Naphazoline is a Non-selective Alpha Agonist.

It is mainly used to treat nasal congestion by causing vasoconstriction in the upper respiratory.

Pateints may build up a tolerance after prolonged use and might experience rebound nasal congestion after discontinuing the drug.
Clonidine
Clonidine is a Centrally Acting Alpha-2 Selective Agonist.

This drug is mainly used to lower blood pressure by decreasing sympathetic neurotransmission from the CNS, which leads to a decrease in vascular resistance.

Common side-effects may include: dry mouth and sedation.
Tizanadine
Tizanadine is a Centrally Acting Alpha-2 Selective Agonist.

It is useful for its effects on reducing muscle spasticity due to presynaptic inhibition of motor neurons via activation of alpha-2 autoreceptors. Overall this leads to a decrease in muscle tone and relief of muscle spasticity.
Dobutamine
Dobutamine is a Beta-1 Selective Adrenergic Agonist, but is now thought to also activate alpha-1 receptors in the heart.

This drug will increase heart contractility (inotropic) and not HR. It is used parenterally as a vasopressor drug for short-term emergency management of cardiac decompensation.

Possible side-effects include: anxeity and nervousness.
Albuterol
Albuterol is a Beta-2 Selective Agonist.

It is a short-term treatment of COPD and is usually given via areosol to cause bronchodilation.

Doses high enough can cause an increase in HR and contractility. Side-effects include tachycardia and muscle tremors.

It contains a hydroxymethyl group that increases its beta-2 selectivity and prevents metabolism by COMT.
Levalbuterol
Levalbuterol is a Beta-2 Selective Agonist.

It is a short-term treatment of COPD and is usually given via areosol to cause bronchodilation.

Doses high enough can cause an increase in HR and contractility. Side-effects include tachycardia and muscle tremors.

It contains a hydroxymethyl group that increases its beta-2 selectivity and prevents metabolism by COMT.
Metaproterenol
Metaproterenol is a Beta-2 Selective Agonist.

It is a short-term treatment of COPD and is usually given via areosol to cause bronchodilation.

Doses high enough can cause an increase in HR and contractility. Side-effects include tachycardia and muscle tremors.

This drug is able to aviod metabolism by COMT
Pirbuterol
Pirbuterol is a Beta-2 Selective Agonist.

It is a short-term treatment of COPD and is usually given via areosol to cause bronchodilation.

Doses high enough can cause an increase in HR and contractility. Side-effects include tachycardia and muscle tremors.
Salmeterol
Salmeterol is a Beta-2 Selective Agonist.

It is a long-term treatment of COPD and is usually given via areosol to cause bronchodilation.

Doses high enough can cause an increase in HR and contractility. Side-effects include tachycardia and muscle tremors.

The addition of a long carbon-based chain onto the amine position results in its long acting.
Amphetamine
Amphetamine is a CNS stimulant that promotes the release of norepi from presynaptic storage vescles.

It is used for the treatment of ADHD (Adderall). But is frequently abused due to its ability to cause feelings of euphoria and increased energy.
Methylphenidate
Methylphenidate is a CNS stimulant that promotes the release of norepi from presynaptic storage vescles.

It is used for the treatment of ADHD (Ritalin).
Phentermine
Phentermine is a CNS stimulant that promotes the release of norepi from presynaptic storage vescles.
Epinephrine
Epinephrine is a neurotransmitter that is released form the adrenal medulla and activates adrenergic receptors.

The addition of a short carbon chain onto the amine position (not having a NH2 at the end) increases its selectivity for beta receptors.

When given as an IV or IM bolus dose epi can cause rapid short-term increase in BP, and can be used during shock. This is due to an increase in HR, contractility, and vasoconstriction (alpha-1), and is referred to as a "pressor" agent.

At lower doses, epi may actually cause overall vasodilation
Norepinephrine
Norepinephrine is a neurotransmitter released by postsynaptic nerve terminals. It mainly binds to alpha and beta-1 receptors.

Norepi is most commonly used as a vasopressor due to its activity on alpha-1 receptors and does significantly increase cardiac output.

Since it dose not effect beta-2 receptors vasodilation at lower doses does not occur.

Norepi and Epi increase glycogenolysis in the liver leading to increased blood sugar.
Carvedilol
Carvedilol is a Non-Selective Adrenergic Antagonist.

This drug causes vasodilation and a decrease in BP, but generally without reflex tachycardia, due to the fact that it also simultaneously blocks beta-1 receptors in the heart.

It is used to treat hypertension and CHF.
Labetalol
Labetalol is a Non-Selective Adrenergic Antagonist.

This drug causes vasodilation and a decrease in BP, but generally without reflex tachycardia, due to the fact that it also simultaneously blocks beta-1 receptors in the heart.

It is used to treat hypertension and CHF.
Doxazosin
Doxazosin is a Alpha-1 Selective Adrenergic Antagonist. It belongs to the quinazolines and is highly selective competitive inhibitors of alpha-1 receptors.

It causes potent peripheral vasodilation which reduces BP. And can also be useful in the treatment of BPH by blocking contraction of the prostate.

It can be given along with Epi, in doing so the drug will block alpha-1 causing Epi to move to beta-2 and activate it causing vasodilation.

Patients may lose consciousness after the first dose (1st dose syncope)
Terazosin
Terazosin is a Alpha-1 Selective Adrenergic Antagonist. It belongs to the quinazolines and is highly selective competitive inhibitors of alpha-1 receptors.

It causes potent peripheral vasodilation which reduces BP. And can also be useful in the treatment of BPH by blocking contraction of the prostate.

It can be given along with Epi, in doing so the drug will block alpha-1 causing Epi to move to beta-2 and activate it causing vasodilation.

Patients may lose consciousness after the first dose (1st dose syncope
Alfuzosin
Alfuzosin is a Alpha-1 Selective Adrenergic Antagonist. It belongs to the quinazolines and is highly selective competitive inhibitors of alpha-1 receptors.

It causes potent peripheral vasodilation which reduces BP. And can also be useful in the treatment of BPH by blocking contraction of the prostate.

It can be given along with Epi, in doing so the drug will block alpha-1 causing Epi to move to beta-2 and activate it causing vasodilation.

Patients may lose consciousness after the first dose (1st dose syncope
Tamsulosin
Tamsulosin is a Alpha-1A Selective Antagonist. This drug is used specifically to treat BPH.
Sotalol
Sotalol is a Non-Selective Beta Adrenergic Antagonist.

It can cause a decrease in production of aqueous humor, decreasing intraocular pressure. Used to treat Glaucome.

It decreases HR and contractility. By inhibiting beta-2 it may cause a slight increase in TPR due to prevention of beta-2 vasodilation.

This drug is especially useful in treating cardiac arrythmias.

This drug may increase airway resistance and secretions. So patients with COPD use caution.

Side-effects include: CNS depression, sleep disorders, fatigue.
Propranolol
Propranolol is a Non-Selective Beta Adrenergic Antagonist.

It can cause a decrease in production of aqueous humor, decreasing intraocular pressure. Used to treat Glaucome.

It decreases HR and contractility. By inhibiting beta-2 it may cause a slight increase in TPR due to prevention of beta-2 vasodilation.

This drug is especially useful in treating cardiac arrythmias.

This drug may increase airway resistance and secretions. So patients with COPD use caution.

Side-effects include: CNS depression (greatest), sleep disorders, fatigue.
Timolol
Timolol is a Non-Selective Beta Adrenergic Antagonist.

It can cause a decrease in production of aqueous humor, decreasing intraocular pressure. Used to treat Glaucome.

It decreases HR and contractility. By inhibiting beta-2 it may cause a slight increase in TPR due to prevention of beta-2 vasodilation.

This drug may increase airway resistance and secretions. So patients with COPD use caution.

Side-effects include: CNS depression, sleep disorders, fatigue.
Pindolol
Pindolol is a Non-Selective Beta Adrenergic Antagonist.

It can cause a decrease in production of aqueous humor, decreasing intraocular pressure. Used to treat Glaucome.

It decreases HR and contractility. By inhibiting beta-2 it may cause a slight increase in TPR due to prevention of beta-2 vasodilation.

This drug may increase airway resistance and secretions. So patients with COPD use caution.

Side-effects include: CNS depression, sleep disorders, fatigue.
Nadolol
Nadolol is a Non-Selective Beta Adrenergic Antagonist.

It can cause a decrease in production of aqueous humor, decreasing intraocular pressure. Used to treat Glaucome.

It decreases HR and contractility. By inhibiting beta-2 it may cause a slight increase in TPR due to prevention of beta-2 vasodilation.

This drug may increase airway resistance and secretions. So patients with COPD use caution.

Side-effects include: CNS depression, sleep disorders, fatigue.
Atenolol
Atenolol is a Beta-1 Selective Antagonist. It has a chemical substituent in the para position of the aromatic ring that gives it beta selectivity.

This drug is used to decrease HR, contractility, and BP. And it has fewer adverse effects that non-selective beat blockers.

There is a slight chance that in a increase in airway resistance and secretions.

It could possible cause CNS depression. Also beta antagonists partially inhibit glycogenolysis in the liver and may decrease insulin secretion.
Betaxolol
Betaxolol is a Beta-1 Selective Antagonist. It has a chemical substituent in the para position of the aromatic ring that gives it beta selectivity.

This drug is used to decrease HR, contractility, and BP. And it has fewer adverse effects that non-selective beat blockers.

There is a slight chance that in a increase in airway resistance and secretions.

It could possible cause CNS depression. Also beta antagonists partially inhibit glycogenolysis in the liver and may decrease insulin secretion.
Bisoprolol
Bisoprolol is a Beta-1 Selective Antagonist. It has a chemical substituent in the para position of the aromatic ring that gives it beta selectivity.

This drug is used to decrease HR, contractility, and BP. And it has fewer adverse effects that non-selective beat blockers. And is used in patients with CHF.

There is a slight chance that in a increase in airway resistance and secretions.

It could possible cause CNS depression. Also beta antagonists partially inhibit glycogenolysis in the liver and may decrease insulin secretion.
Metoprolol
Metoprolol is a Beta-1 Selective Antagonist. It has a chemical substituent in the para position of the aromatic ring that gives it beta selectivity.

This drug is used to decrease HR, contractility, and BP. And it has fewer adverse effects that non-selective beat blockers.

There is a slight chance that in a increase in airway resistance and secretions.

It could possible cause CNS depression. Also beta antagonists partially inhibit glycogenolysis in the liver and may decrease insulin secretion.
Esmolol
Esmolol is a Beta-1 Selective Antagonist. It has a chemical substituent in the para position of the aromatic ring that gives it beta selectivity.

This drug is used to decrease HR, contractility, and BP. And it has fewer adverse effects that non-selective beat blockers. And is also useful in treating cardiac arrythmias. And can be used for short-term control of life-threatening hypertension.

There is a slight chance that in a increase in airway resistance and secretions.

It could possible cause CNS depression. Also beta antagonists partially inhibit glycogenolysis in the liver and may decrease insulin secretion.