3B Autonomic drugs

agonist or antagonist

• bind to the receptor on the tissue
• maximal, where it's excitatory or inhibitory

• Bind to receptors and block and reverse the effects of the neurotransmitter
• submaximal

• adrenergic agonists
• mimic/increase sympathetic function

• adrenergic blockers, sympathetic blockers
• these block/stop sympathetic function

• cholinergic agonists
• mimic or increase parasympathetic function

• anticholinergic agents, or cholinergic blockers
• block or stop parasympathetic function

cardiovascular

• Direct acting
• Indirect acting

bind directly to and activate the alpha or beta receptors, imitating the action of the neurotransmitter

do not themselves bind to the receptor, but cause release of NE from the nerve terminals. Then, the NE interacts with the receptor site

smooth muscles of the blood vessels supplying organs such as the heart, skin, and salivary glands and smooth muscle of the eye, glands, GI tract, and urinary bladder

vasoconstriction, dilation of the pupils (let’s more light in), and contraction of isolated smooth muscle

the intestine leads to intestinal relaxation

–Located on the terminals of neurons that are releasing NE. Many are centrally located - i.e. in the CNS

reduces further NE release

• Located on heart muscle
• increased heart rate

• Located on smooth muscle of the bronchioles (lungs) and intestines, and bloods vessels supplying the heart
• relaxation of smooth muscle

alpha and beta

vasoconstrictor

Powerful cardiac stimulant used in heart failure

Powerful relaxation of smooth muscle in the lungs with bronchodilation. Used in severe asthmatic emergency

prolong the localized activity of agent through vasoconstriction

• Beta-2
• vasodilation of skeletal and smooth muscle causing a decrease in diastolic blood pressure

an increase in cardiac output resulting in an increase in systolic blood pressure

• Neo-Cobefrin
• Vasoconstrictor used in local anesthetic agents. 
• alpha1 interaction with little or no effect on the Beta adrenergic receptors

• Neo-Synephrine
• Causes vasoconstriction. Used in nasal sprays where it shrinks vessels in stuffy nose opening airway. Rebound effect leads to “nose spray junkies”.

• CNS (brain)
• by stimulating the alpha2 (preganglionic) receptors
• sympathetic outflow of NE from the nerve terminals. Works like blockers (antagonists).

lower blood pressure due to less norepinephrine being released

• Catapres
• prototype of central 2 agonist
• used to lower blood pressure

• in the treatment of bronchial asthma
•  B2-adrenergic receptors
• causing dilation of the bronchial smooth muscle and vasoconstriction of the bronchial blood vessels

• Isuprel
• prototype of Beta 1/Beta 2 Adrenergic Agonist.
• Nonselective so it acts on both B1 and B2 receptors therefore it also affects the heart by causing increased heart rate (B1)

• Ventolin, Proventil
• specific beta2 agonist. Opens lung passages. Used in rescue inhalers for asthma. Since it is selective for B2, there are less effects on the heart

• Adderall
• lipophilic drug w/powerful CNS effects leading to huge catecholamine release. Leads to increased alertness, relief of fatigue, euphoria, increased number of errors. - increases release of dopamine in the synaptic cleft

naturally occurring, the most potent vasoconstrictor, used as a local anesthetic. Adrenergic effects include cardiac stimulation and elevation of blood pressure

• Ritalin
• Used to treat ADHD and narcolepsy. Prevents reuptake of dopamine from the synaptic cleft.
• These drugs are abused by high school and college students who purchase these agents for “help” on exams

• Sudafed
• Used as nasal decongestant
• These are also used for the illicit manufacture of methamphetamine. Therefore, consumers can only buy 3.6 grams in one day, and a total of 9 grams per month

“Meth” is more lipid soluble w/ more CNS activity. Leads to huge central release of neurotransmitters causing euphoria and excitement. Tremendous addictive potential

α1-receptor agonists cause smooth muscle contraction, which leads to vasoconstriction, dilation of the pupils, and contraction of the bladder muscle. These drugs are used in the treatment of shock and hypotension and as a nasal/ocular decongestant

α2-receptor agonists are used in the treatment of hypertension to lower blood pressure. These drugs will inhibit the release of NE, resulting in lower levels of NE

β1-receptor agonists are used to increase the rate and force of heart contractions (cardiac stimulation) in patients with hypotension and shock. These drugs are given intravenously

β2-receptor agonists are used to cause relaxation or dilation of smooth muscle in the lungs (bronchodilation) in patients with asthma. These long-acting drugs are given orally or inhaled. It is best to choose a selective β2 drug such as albuterol (Ventolin, Proventil) or terbutaline (Brethine) to keep adverse side effects to a minimum

reuptake of catecholamines and may increase the hypertensive effects of epinephrine

directly (competitively) block alpha or beta receptors

• block sympathetic stimulation of alpha1 preventing the contraction of smooth muscle in the vessels of the skin or along the course of the urethra
• lowering blood pressure and making it easier to urinate in benign prostatic hyperplasia (BPH)

"zosin"

• Minipres
• hypertension

• Cardura
• hypertension

• Hytrin
• hypertension, prostate hypertrophy, urinary retention

• Flomax
• Prostate hypertrophy

patients can get faint or dizzy when moving the chair from a supine to an upright position due to orthostatic hypotnsion. Keep the patient from getting up for a few minutes to prevent a fall

both beta1 and beta2, or are selective for one or the other

olol

—cardiovascular disease such as hypertension, angina, and heart arrhythmias as well as panic attacks, migraine headaches, glaucoma

bronchospasm, bradycardia, and hypoglycemia

• Inderal
• is the prototype non-selective B blocker. Used to treat hypertension by decreasing cardiac output and blood pressure

• Tenormin
• hypertension

• Lopressor
• hypertension

• Coreg
• More commonly encountered. Blocks both beta2 and alpha1 receptors treating hypertension and atrial fibrillation

• Cardiovascular: Decrease rate and force of heart beat through vagus nerve activation
• GI/Urinary Tract: Increase in muscle contraction (peristalsis), muscle tone, and secretions (including salivary flow)
• Eye: Miosis (constriction of pupil)

• Direct Acting Cholinergic Agonists
• Indirect Acting Cholinergic Agonists– also referred to as cholinesterase inhibitors

has almost no clinical use because it is rapidly destroyed and causes many adverse effects

• Urecholine
• Prevents urinary retention and increases intestinal motility after surgery

• Salagen
• Treats xerostomia usually in head and neck radiation and Sjogren’s syndrome by increasing saliva (sialogogue). Treats glaucoma by decreasing intraocular pressure

• Evoxac
• Drug for xerostomia that is more specific to receptors on salivary glands therefore has fewer side effects

• Cognex
• Treats Alzheimer’s disease

• Aricept
• Treats Alzheimer’s disease

(insecticide)- irreversible binding to AChase

(nerve gas) -irreversible binding to AChase

motion sickness, dispensed in transdermal patch

used in dentistry to create xerostomia and a dry operative field

• Detrol
• increases bladder volume, used to treat incontinence

• Ditropan
• antispasmodic action on bladder muscle decreasing urge to void

xerostomia (cevimeline, pilocarpine) and Alzheimer’s disease (donepezil, tacrine, rivastigmine)

increase heart rate (atropine) and to treat urinary incontinence (oxybutynin), motion sickness (scopolamine), and irritable bowel syndrome (dicyclomine, propantheline, scopolamine)

of their numerous side effects.

• scopolamine
• atropine
• tolterodine (Detrol)
• oxybutynin (Ditropan)

• tacrine (Cognex) – Treats Alzheimer’s disease.
• donepezil (Aricept) – Treats Alzheimer’s disease
• malathion (insecticide) - irreversible binding to AChase
• sarin (nerve gas) -   irreversible binding to AChase

• acetylcholine (Ach)– (prototype) has almost no clinical use because it is rapidly destroyed and causes many adverse effects
• bethanechol (Urecholine)– Prevents urinary retention and increases intestinal motility after surgery
• pilocarpine (Salagen) – Treats xerostomia usually in head and neck radiation and Sjogren’s syndrome by increasing saliva (sialogogue). Treats glaucoma by decreasing intraocular pressure
• cevimeline (Evoxac)– Drug for xerostomia that is more specific to receptors on salivary glands therefore has fewer side effects
• Nicotine – used for smoking cessation

carvedilol (Coreg) – second drug of its class. More commonly encountered. Blocks both beta2 and alpha1 receptors treating hypertension and atrial fibrillation

• atenolol (Tenormin) - hypertension
• metoprolol (Lopressor) – hypertension

propranolol (Inderal) – is the prototype non-selective B blocker. Used to treat hypertension by decreasing cardiac output and blood pressure

• prazosin (Minipres) - hypertension
• doxazosin (Cardura) - hypertension
• terazosin (Hytrin) – hypertension, prostate hypertrophy, urinary retention
• tamsulosin (Flomax) – Prostate hypertrophy

• ephedrine and pseudoephedrine (Sudafed). Used as nasal decongestant. These are also used for the illicit manufacture of methamphetamine. Therefore, consumers can only buy 3.6 grams in one day, and a total of 9 grams per month
• methamphetamine - “Meth” is more lipid soluble w/ more CNS activity. Leads to huge central release of neurotransmitters causing euphoria and excitement. Tremendous addictive potential. Meth high lasts much longer than using crack (1 hour vs. 12).

• amphetamine (Adderall)– lipophilic drug w/powerful CNS effects leading to huge catecholamine release. Leads to increased alertness, relief of fatigue, euphoria, increased number of errors. - increases release of dopamine in the synaptic cleft
• cocaine – naturally occurring, the most potent vasoconstrictor, used as a local anesthetic. Adrenergic effects include cardiac stimulation and elevation of blood pressure
• methylphenidate (Ritalin) Used to treat ADHD and narcolepsy. Prevents reuptake of dopamine from the synaptic cleft.

• isoproterenol (Isuprel)- is the prototype for Beta 1 /Beta 2 Adrenergic Agonists. Drugs used in the treatment of bronchial asthma affect the B2-adrenergic receptors. Causes dilation of the bronchial smooth muscle and vasoconstriction of the bronchial blood vessel. Nonselective so it acts on both B1 and B2 receptors therefore it also affects the heart by causing increased heart rate (B1).
• albuterol (Ventolin, Proventil)– specific beta2 agonist. Opens lung passages. Used in rescue inhalers for asthma. Since it is selective for B2, there are fewer effects on the heart

• levonordefrine (Neo-Cobefrin): Vasoconstrictor used in local anesthetic agents. Unlike epinephrine, has mostly alpha1 interaction with little or no effect on the Beta adrenergic receptors.
• phenylephrine (Neo-Synephrine)– Alpha1 agonist. Causes vasoconstriction. Used in nasal sprays where it shrinks vessels in stuffy nose opening airway. Rebound effect leads to “nose spray junkies”.