Autonomic Drugs
Autonomic Drugs
Autonomic Drugs
Parasympathetic Receptors
Three types of receptors in the parasympathetic system a. muscarinic b. nicotinic C. somatic-skeletal muscle
PANS
Action potential travels along the nerve
Causes release of Ach
Note: Atropine can block the action of acetylcholine at the post gang endings but not at the neuromuscular junction this is part of the ANS but not what we are concerned with.
Cholinergic agents
Cardiovascular effects
Direct effect
Decrease in cardiac output. Negative chronotropic and inotropic effect
Chronotropic effect = rate Inotropic effect = force of contractility of the heart muscle
Smooth muscle around the blood vessels results in relaxation and vasodilation Decrease in total peripheral resistance
Indirect effect
Increase in heart rate and cardiac output Positive chronotropic and inotropic effect
Eye
Cholinergic agents
Cause cycloplegia - paralysis of the ciliary muscle of the eye so that it results in loss of visual accommodation Effect - Miosis
Constricted pupil
Indirect acting
Causes release of neurotransmitter
Cholinesterase inhibitors (inhibit that exzyme) Reversible cholinesterase inhibitors Used to treat glaucoma and myasthenia gravis Rate of reversibility is based on the enzyme binding Concentration of acetylcholine builds up = P stimulation Irreversible cholinesterase inhibitors Developed for chemical warfare and pesticides
pilocarpine - Salagen
Cholinergic agent Treatment of xerostomia Side effects
Sweating Nausea Chills, flushing Rhinitis
Slowly reversible
Physostigmine and neostigmine
Sarin (used to poison subway riders in Japan. Used for chemical warfare.
Parasympatholytic/Anticholinergic Agents
Anticholinergic Drugs
blocks receptor site for acetylcholine Causes a decrease salivary flow and respiratory secretions during surgery Aka: antimuscarinic agents
Parasympatholytic/Anticholinergic Agents
CNS
Depending on dose can stimulate/depress
Pg. 41
Exocrine glands
Reduce flow and volume of secretions Used therapeutically in dentistry to decrease salivation
Smooth muscle
Relax smooth mus. in respiratory and GI tract
Meds are also called, spasmolytic agents Used to slow down the GI tract Used to treat asthma
Parasympatholytic/Anticholinergic Agents
Eye
Mydriasis
Dilation of pupil
Cyclopegia
Paralysis of the eye that results in the loss of visual accommodation
Parasympatholytic/Anticholinergic Agents
Cardiovascular
Large doses
Tachycardia
Used to prevent cardiac slowing during general anesthesia Produces vagal blockade = tachycardia
Small doses
Bradycardia predominates
Parasympatholytic/Anticholinergic Agents
Adverse Reactions
Extensions of their pharmacologic effects
Xerostomia Blurred vision and photophobia (sens to light) Tachycardia GI stasis and Urinary tract stasis
Peristalsis and urination stops Constipation
Parasympatholytic/Anticholinergic Agents
Contraindications
Glaucoma
Can cause acute rise in intraocular pressure
Prostatic hypertrophy
Men who have difficulty urinating already should not be given drug, may need catheter
Intestinal/Urinary blockage
People already constipated/urinary tract retention
CV Disease
Why? Because anticholinergic agents can block the vagus nerve and result in tachycardia
Parasympatholytic/Anticholinergic Agents
Uses
Preoperative medication
Reduce saliva Ability to block the vagal slowing of the heart that results from general anesthesia
Parasympatholytic/Anticholinergic Agents
Uses
Eye exam
Mydriasis and cyclopegia (relax the lens of eye)
Motion Sickness
Scopolamine
CNS depression
Parasympatholytic/Anticholinergic Agents
Atropine a. decreases secretions and salivation b. adverse reactions --increase heart rate without increased cardiac output --red, mad, hot c. dose range in 0.2 to l.0mg --usually ranges from 0.4 to 0.6mg d. contraindicated in glaucoma and, over long term, among patients with prostatic hypertrophy
ANS Part 2
PARASYMPATHETIC
cholinergic the body at ease mediator:
acetylcholine
the "mediator" listed above refers to that magic neurotransmitter at the synapse
Its neurotransmitters are epinephrine and norepinephrine. Dopamine receptors in the brain, splanchnic (viscera-i.e.-abdominal organs) and renal vasculature are important
originate from
Thoracic (T1) to the lumbar (L2) Produces a more diffuse effect Fibers exit the cord, enter the sympathetic chain, form multiple synaptic connections
SANS
Pre
Indirect action
Amphetamine, release endogenous NE = response
Mixed action
Agents such as ephedrine, stimulate the receptor directly to release endogenous NE to cause a response
SANS Receptors
Alpha receptors
Stimulation
Results in smooth muscle excitation or contraction
Causes vasoconstriction Drugs that block the alpha receptors are called a-adrenergic blocking agents
SANS Receptors
Beta receptors
Two types
Beta 1 Beta 2
SANS Receptors
Beta 1 receptor
Controls the heart
(you have only 1 heart)
SANS Receptors
Beta 2
Stimulation
Smooth-muscle inhibition or relaxation
Relaxation of bronchioles with beta2 receptors
SANS Receptors
Agents that block the effects
Beta-adrenergic blocking agents Some drugs will block both beta 1 and beta 2 receptors
i.e. propranolol
Beta Receptors
Drugs that block -receptor effects are called adrenergic blocking agents
Some are nonspecific, blocking both 1- and 2-receptors Others are more selective, blocking primarily 2-receptors
Play important role in treating anaphylaxis and asthma Added to local anesthetics
vasoconstrictors
NE
Primarily stimulates alpha receptors
Isoproterenol
Acts mainly on beta receptors
Vessels
Depends on location
Innervated by alpha or beta or both Alpha = vasoconstriction in skin and mucosa Beta = vasodilation of skeletal muscle
NE
Rise in both systolic and diastolic pressures
Isoproterenol
Little change in systolic, decrease in diastolic
Isoproterenol, primarily a -agonist, produces vasodilation that triggers an increase in heart rate (vagal reflex)
Mydriasis
Respiratory
Relax the bronchiole smooth muscle
Useful in treating asthma
Metabolic rate
Increases basal metabolic rate
Hemostasis
Stops bleeding, infiltrate locally
In retraction cord
Decongestion
In nose drops
Constrict vessels, reduce swelling of mucous membranes of nose. Repeated use? Rebound congestion will occur Symptoms greater than before
Emphysema
CNS Stimulation
Amphetamine-like agents
Diet
phenylephrine (Neo-Synephrine) a. stimulates alpha receptors b. similar to epinephrine without cardiac effects c. has been used with local anesthetics d. in eye, for dilation of pupil for examination (pupil dilation--MYDRIASIS) e. main claim to fame: nasal decongestant, drops or spray, 0.25-1% solution, or as a jelly for small children
dipivefrin (Propine)
Used to tx glaucoma
REVIEW!!!!!
Cholinergic Pharmacology
Cholinergic Pharmacology
Cardiovascular
Direct effects include negative chronotropic and inotropic actions. Relaxation of smooth muscles causes a decrease in total peripheral resistance. Indirect effects include increased heart rate and cardiac output. The resulting effect depends upon the dose used. Usually, the patient experiences bradycardia and a decrease in blood pressure and cardiac output.
Cholinergic Pharmacology
Cholinergic Pharmacology
Gastrointestinal
These drugs excite the smooth muscle of the gastrointestinal tract and cause an increase in activity, motility, and secretion.
Eye
These drugs cause miosis and cycloplegia. They cause a decrease in intraocular pressure.
Cholinergic Pharmacology
Adverse Reactions
Adverse reactions are an extension of the drugs pharmacologic effects. They include:
Salivation Lacrimation Urination Defecation Paralysis Overdose
Cholinergic Pharmacology
Contraindications
The contraindications and relative cautions are a result of the drugs pharmacologic and adverse effects. They include:
Bronchial asthma Hyperthyroidism Gastrointestinal or urinary tract obstruction Myasthenia gravis treated with neostigmine Peptic ulcer disease Severe cardiac disease
Anticholinergic Drugs
These drugs prevent the action of acetylcholine at postganglionic parasympathetic endings. Acetylcholine is released but its receptor site is completely blocked by anticholinergic drugs. These drugs only block muscarinic receptors
Anticholinergic Drugs
Pharmacology
Central Nervous System
Depending on the dose, these drugs can cause stimulation or depression.
Exocrine Glands
They reduce the flow and volume of secretions in the respiratory, gastrointestinal, and genitourinary tracts.
Anticholinergic Drugs
Pharmacology
Central Nervous System
Depending on the dose, these drugs can cause stimulation or depression.
Exocrine Glands
They reduce the flow and volume of secretions in the respiratory, gastrointestinal, and genitourinary tracts
Anticholinergic Drugs
Pharmacology
Cardiovascular
With large doses, these drugs produce vagal blocking which results in tachycardia. Bradycardia can occur with low doses.
Anticholinergic Drugs
Adverse Reactions
The adverse reactions are an extension of the drugs pharmacologic effects. They include:
Xerostomia Constipation Urinary retention Blurred vision Hyperpyrexia Hallucinations Photophobia Tachycardia
Anticholinergic Drugs
Contraindications
Contraindications are usually due to the drugs pharmacologic and adverse effects. They include:
Glaucoma Prostatic hypertrophy Intestinal or urinary obstruction or retention Cardiovascular disease
Anticholinergic Drugs
Uses
Preoperative Medication
They inhibit salivary and bronchial secretions. They block the vagal slowing of the heart that can occur with general anesthesia.
Gastrointestinal Disorders
They decrease gastrointestinal motility and can be used to treat ulcers, diarrhea, and hypermotility.
Anticholinergic Drugs
Uses
Ophthalmologic Examinations
Topical use can cause mydriasis which causes a full visualization of the retina. Cycloplegia relaxes the lens so that proper prescriptions for glasses can be determined.
Parkinson Disease
They reduce the tremors and rigidity associated with Parkinson and drug-induced Parkinson disease.
Anticholinergic Drugs
Uses
Motion Sickness
These drugs are used to treat or prevent motion sickness because of their central nervous system depressant action.
Dentistry
These drugs are used to create a dry, oral field.
Please! NO MORE!
Adrenergic Drugs
Adrenergic drugs can be classified as having direct action, indirect action, or mixed action. These drugs stimulate and receptors throughout the body. Drugs with direct action (epinephrine, norepinephrine, isoproterenol) produce their effect by directly stimulating the receptor site. Drugs with indirect action (amphetamine) release endogenous norepinephrine which then stimulates the receptor. Drugs with mixed action (ephedrine) either directly stimulate the receptor or release endogenous norepinephrine.
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Adrenergic Drugs
Pharmacology
Central Nervous System (CNS)
These drugs produce CNS excitation or alertness. Higher doses produce anxiety, apprehension, restlessness, and tremors.
Cardiovascular System
These drugs increase the force and rate of contraction of the heart. Blood pressure is also increased. Total peripheral resistance is also increased.
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Adrenergic Drugs
Pharmacology
Eye
These drugs lower intraocular pressure and can cause mydriasis.
Respiratory System
These drugs cause a relaxation of bronchiole smooth muscles.
Metabolic Effects
Increased glycogenolysis from -receptor stimulation causes hyperglycemia.
Salivary Glands
These drugs produce vasoconstriction of the salivary glands which leads to decreased salivary flow which results in xerostomia.
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Adrenergic Drugs
Adverse Reactions
The adverse reactions associated with these drugs are an extension of the drugs pharmacologic effects. They include:
Anxiety Tremors Tachycardia Increased blood pressure Arrhythmias
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Adrenergic Drugs
Uses
Vasoconstriction
These drugs are used in dentistry because of their vasoconstrictive actions on blood vessels. They are added to local anesthetics because they prolong the action of the local anesthetic, reduce the risk for systemic toxicity, and help to create a dry field.
Cardiac Effects
These drugs are used to raise blood pressure and to treat cardiac arrest.
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Adrenergic Drugs
Uses
Bronchodilation
These drugs are used to treat asthma, emphysema, and allergic reaction.
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Antiadrenergic Drugs
Pharmacology
These drugs reduce sympathetic tone in the blood vessels and decrease total peripheral resistance. This results in a reduction in blood pressure.
Uses
These drugs are used to treat hypertension, peripheral vascular disease (i.e., Raynaud syndrome) and benign prostatic hypertrophy.
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