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Which drug class is Epinephrine in?
Sympathetic Agonists - Nonspecific
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List the indications for Epinephrine
- Local Vasoconstriction
- Hypotension and Shock
- Bronchodilation
- Allergy
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What is the mechanism of action of Epinephrine?
Direct stimulation of α and β adrenergic receptors
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How is Epinephrine used in dentistry?
Vasoconstriction—less bleeding and makes the analgesia last longer
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Use of Epinephrine could result in complications/ adverse effects in patients with what types of medical conditions?
- Cardiac disease
- Cerebrovascular disease
- Diabetes
- Parkinson's disease
- Thyroid disease
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What is the impact of Epinephrine on the heart?
β1 stimulation increases the work of the heart and decreases cardiac efficiency
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What effects of Epinephrine are of concern in the diabetic patient?
- Increases in circulating blood glucose from stimulation of liver glycogenolysis and glucagon secretion
- Inhibition of insulin secretion
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Why is the use of Epinephrine a cause for concern in patients with Parkinson's disease?
May cause temporary worsening of symptoms
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What is the upper limit of Epinephrine that can be used, per procedure, in patients taking β-Blockers?
Upper Limit: 0.04 mg total per procedure
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Epinephrine can adversely interact with what types of medications?
- Tricyclic Antidepressants
- β-Blockers
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What adverse effects can be seen if Epinephrine is given to a patient on Tricyclic Antidepressants?
Tricyclic Antidepressants block reuptake and degradation of epi, leading to more cardiac adverse effects
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What adverse effects can be seen if Epinephrine is given to a patient on Non-Selective β-Blockers?
Block β receptors in the peripheral blood vessels, epi acts as a pure α agonist and blood pressure rises
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What adverse effects can be seen if Epinephrine is given to a patient on Selective β-Blockers?
Selective Block β1 receptors in heart, at high doses block β 2 receptors in peripheral blood vessels
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Name two α Sympathetic Agonists
- Methylphenidate (Ritalin)
- Amphetamine (Adderall)
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What is the mechanism of action of α Sympathetic Agonists?
Release of Norepi from synaptic vesicle
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What are α Sympathetic Agonists used for?
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What is the risk for abuse and addiction of α Sympathetic Agonists?
Schedule 2 (Ritalin and Adderall)
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What are the adverse effects of α Sympathetic Agonists?
- Dyskinesia, muscle tightness, bruxism
- The FDA asked the Drug Safety and Risk Management advisory committee to look into studying the cardiac risk in both adult and children taking ADHD drugs
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Which drug class is Clonidine (Catapres) in?
Presynaptic α2 Agonist
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What is Clonidine (Catapres) used for?
- Used in hypertension (oral tablet and patch)
- Used with opiates to relieve the pain associated with end-stage cancer (Epidural Injection)
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What is the mechanism of action of Clonidine (Catapres)?
- Inverse Agonist
- Binds to α2 medullary receptors in the brain which inhibit sympathetic outflow to the body and α receptors in blood vessels are inhibited
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What are the Dental Adverse Effects of Clonidine (Catapres)?
- Dry mouth
- Orthostatic hypotension
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What dosage forms is Clonidine (Catapres)
available in?
Oral Tablet: Used for HTN
Patch: Used for HTN (Catapres TTS)
Epidural Injection: Used with opiates to relieve the pain associated with end-stage cancer
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Which drug class is Albuterol (Proventil) in?
β2 Sympathetic Agonist
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What is Albuterol (Proventil) used for?
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What is the mechanism of action of Albuterol (Proventil)?
Stimulation of β2 receptors in lungs to cause bronchodilation
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What dosage forms is Albuterol (Proventil) available in?
- Albuterol Inhalation Aerosol
- Note: when inhaled, β2 receptors in the lungs will receive most of the drug to decrease the chance for adverse effects
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What are the Dental Adverse Effects of Albuterol (Proventil)?
- unusual taste
- drying or irritation of the oropharynx
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What are the effects of Acetylcholine?
- Bradycardia
- Vasodilation
- Bronchoconstriction
- Relaxation of urinary sphincter
- Increase GI secretions
- Sweating
- Contraction of iris
- SLUD Response: Salivation, Lacrimation, Urination, Defecation
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What are the therapeutic uses of drugs at Adrenegeric Receptors (Antagonists)?
- HTN
- Post myocardial infarction
- CHF
- Treatment of arrhythmias
- Ischemic heart disease
- Benign prostatic hyperplasia
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Which drug class is Terazosin (Hytrin) in?
α Sympathetic Antagonist
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What is Terazosin (Hytrin) used for?
HTN and benign prostatic hyperplasia
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What is the mechanism of action of Terazosin (Hytrin)?
α1 receptor blockade, leading to smooth muscle relaxation
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What are the Dental Adverse Effects of Terazosin (Hytrin)?
- Dry mouth
- Dizziness
- Orthostatic hypotension
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Which drug class is Tamsulosin (Flomax) in?
α Sympathetic Antagonist
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What is the mechanism of action of Tamsulosin (Flomax)?
Blockade of α1A and α1D adrenergic receptor subtypes found only in prostate gland
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What is Tamsulosin (Flomax) used for?
Benign prostatic hyperplasia
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List eight effects of β Blockers
- ↓ the force and rate of myocardial contraction
- ↓ O2 consumption of the heart
- ↓ of blood pressure in hypertensive patients
- CO decreases
- HR decreases
- Reduction in plasma renin activity
- Decrease CNS sympathetic outflow
- Alteration in baroreceptor responsiveness
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Whate are the 2 types of β Blockers?
- Selective for β1
- Nonselective
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Which drug class is Metoprolol (Toprol XL) in?
β Blocker (Selective for β1)
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What is the mechanism of action of Metoprolol (Toprol XL)?
Competitive inhibitors of epinephrine and norepi at β1
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Which drug class is Propranolol (Inderal) in?
β Blocker (Nonselective)
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What is the mechanism of action of Propranolol (Inderal)?
Non-selective competitive inhibitor of beta receptors
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What is Propranolol (Inderal) used for?
- Cardiovascular Disease
- Stage fright
- Tremor
- Migraine headache
- Sexual aggression
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What are the Dental Adverse Effects of β Blockers?
- Altered taste
- Lichenoid rxns
- Orthostatic hypotension
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What are the Adverse Effects of Non-Selective β Blockers?
- May enhance the pressor response to epinephrine
- Hypertension
- Bradycardia
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Which drug class is Carvedilol (Coreg) in?
β Antagonist
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What is the mechanism of action of Carvedilol (Coreg)?
- Antagonist at β1 and α1 receptors
- Decrease heart rate and contractility and decrease blood pressure through alpha blockade
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What is Carvedilol (Coreg) used for?
CHF (congestive heart failure)
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Name the 4 Mechanisms by which Autonomic Nervous System Drugs Act
- Influence release of the neurotransmitter
- Influence degradation of the neurotransmitter
- Influence reuptake of the neurotransmitter
- Bind (agonist) or block (antagonist) receptor
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Name 2 General Therapeutic Uses of Cholinergic Drugs
- Alzheimer's
- Salivary Stimulants
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Name the 2 mechanisms of Cholinergic Drugs
- Reversible Cholinesterase Inhibition – Prolong t1/2 of acetylcholine at receptor site
- Direct Acting – Bind to and stimulate muscarinic receptors
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Which drug class is Tacrine (Cognex) in?
Cholinesterase Inhibitor
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What is Tacrine (Cognex) used for?
- Alzheimer’s
- Parkinson’s disease with dementia
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What is the mechanism of action of Tacrine (Cognex)?
Idea: Prolong acetylcholine half life in the brain
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Name 2 Salivary Stimulants
- Pilocarpine (Salagen)
- Cevimeline (Evoxac)
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What is the mechanism of action of Salivary Stimulants?
Agonist at muscarinic receptors
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What dosage of Salivary Stimulants is normally prescribed?
Doses are individualized for desired effects until adverse reactions become intolerable.
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Use of Salivary Stimulants could result in complications/ adverse effects in patients with what types of medical conditions?
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Use of Cholinergic Drugs could result in complications/ adverse effects in patients with what types of medical conditions?
Contraindicated in asthma, cardiovascular disease, and ulcer
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What adverse effects are associated with Cholinergic Drugs?
- nausea
- diarrhea
- vomiting
- rhinitis
- urinary frequency
- bronchospasm
- hypotension
- arrhythmias
- (parasympathetic reactions)
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List seven Effects of Norepinephrine
- Tachycardia
- Vasoconstriction
- Bronchodilation
- Contraction of urinary sphincter
- Decreased GI secretions
- Glycogenolysis
- Gluconeogenesis
- Lipolysis
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List five Effects of Antimuscarinic Drugs
- GI:↓ motor and secretory responses
- Eye: Dilation
- Urinary Retention
- Respiratory Tract: Relaxation
- Salivary Glands: ↓ Secretion
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What are the General Therapeutic Uses of Antimuscarinic Drugs?
- Bronchodilation: Asthma and COPD
- Urinary: antispasmodics
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Name 2 Antimuscarinic Drugs used for Bronchodilation (Asthma and COPD)
- Ipratropium (Atrovent)
- Tiotropium (Spiriva)
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Name 2 Antimuscarinic Drugs used to treat urinary disfunction (antispasmodics)
- Tolterodine (Detrol)
- Darifenacin (Enablex)
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What is Ipratropium (Atrovent) used for?
- Bronchodilation
- By itself, or in combination inhalation product with albuterol (Combivent Inhaler)
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What is Tiotropium (Spiriva) used for?
- Bronchodilation
- Prolonged T ½ used primarily in COPD
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Whate are Tolterodine (Detrol) and Darifenacin (Enablex) used for?
- Urinary: “antispasmodics”
- Contracts urinary sphincter muscles used in dysuria, urgency, incontinence
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What is a benefit of Darifenacin (Enablex) vs. Tolterodine (Detrol)?
Darifenacin (Enablex) is a M3 selective agent, less dry mouth and constipation
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What drug interactions are associated with Antimuscarinic Drugs?
- Anticholinergic effects are potentiated by antihistamines. This leads to severe dry mouth.
- CYP2D6 Inhibitors: may diminish the therapeutic effect of Codeine (Enablex)
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List three Therapeutic Uses of Drugs at Nicotinic Receptors
- Only therapeutic use for nicotine: in smoking cessation programs, gum, patches
- Neuromuscular junction blockers are used in surgery and intubation –succinylcholine
- Botulinum toxin type A-Botox
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What is the mechanism of action of Nicotine?
- α4β2 neuronal nicotinic acetylcholine receptors
- stimulate the central nervous mesolimbic dopamine system
- neuronal mechanism underlying reinforcement and reward experienced upon smoking
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What is the mechanism of action of Varenicline (Chantix)?
- α4β2 neuronal nicotinic acetylcholine receptors
- produces agonist activity, while simultaneously preventing nicotine binding to α4β2 receptors
- stimulates receptor-mediated activity, but at a significantly lower level than nicotine
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What are the adverse effects of Varenicline (Chantix)?
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What is the mechanism of action of Botulinum Toxin?
Prevents synaptic vesicle fusion with membrane
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What is Botulinum Toxin used for?
- Focal dystonias
- Headache and pain syndromes
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