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Indications:
Local Vasoconstriction Hypotension and Shock Bronchodilation Allergy
Mechanism:
Direct stimulation of α and β adrenergic receptors
Uses in Dentistry:
Vasoconstriction—less bleeding and makes the analgesia last longer Cardiac: β1 stimulation increases the work of the heart and decreases cardiac efficiency • Cerebrovascular disease: Use with caution in patients with cerebrovascular disease • Diabetes: Increases in circulating blood glucose from stimulation of liver glycogenolysis and glucagon secretion Inhibition of insulin secretion • Parkinson's disease: may cause temporary worsening of symptoms. • Thyroid disease: Use with caution in patients with thyroid disease |
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MOA: α 1 agonist, inhibitor of dopamine reuptake Indication: narcolepsy, shift work disorder Adverse Effects: mania, delusions, hallucinations, suicidal ideation and aggression, persistent sleepiness Not approved for children (risk of Stevens-Johnson Syndrome) |
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Used in hypertension
Mechanism: a2 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
Dental Adverse Effects: Dry mouth, orthostatic hypotension |
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β2 Sympathetic Agonist
Mechanism: Stimulation of β2 receptors in lungs to cause bronchodilation
Use: Asthma, COPD
Dental Adverse Effects: unusual taste, and drying or irritation of the oropharynx
Dosage Form: Albuterol Inhalation Aerosol |
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α Sympathetic Antagonist
Mechanism: α1 receptor blockade, leading to smooth muscle relaxation
Uses: HTN and benign prostatic hyperplasia |
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α Sympathetic Antagonist
Mechanism: Blockade of α1A and α1D adrenergic receptor subtypes found only in prostate gland |
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Pharmacological Effects of β Blockers |
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↓ 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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Nonselective beta blocker
Mechanism: Non-selective competitive inhibitor of beta receptors
Uses: Cardiovascular Disease, Stage fright, Tremor, Migraine headache
may enhance the pressor response to epinephrine hypertension and bradycardia |
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Selective for β1
Mechanism: Competitive inhibitors of epinephrine and norepi at β1
Orthostatic hypotension |
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beta antagonist Mechanism: Antagonist at β1 and α1 receptors
Effects: Decrease heart rate and contractility and decrease blood pressure through alpha blockade
Use: CHF (congestive heart failure) |
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SLUD Response: Salivation Lacrimation Urination Defecation
Bradycardia Vasodilation Bronchoconstriction Relaxation of urinary sphincter Increase GI secretions Sweating Contraction of iris |
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Pilocarpine (Salagen) Cevimeline (Evoxac)
Agonist at muscarinic receptors
Doses are individualized for desired effects until adverse reactions become intolerable.
Contraindicated in asthma, cardiovascular disease, and ulcer
Use with caution in patients with COPD, Parkinson’s disease |
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Bronchodilation: Asthma and COPD: Ipratropium (Atrovent) Tiotropium (Spiriva)
Urinary: antispasmodics Tolterodine (Detrol) Darifenacin (Enablex |
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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
Adverse Effect: Nightmares and psychosis |
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Class: typical antipsychotic
Mechanism: Binds to receptors in all central dopamine pathways
Use: Alleviate positive symptoms of Schizophrenia, hallucinations, delusions. No effect on negative symptoms:
adverse effect: Dystonia-dyskinetic movements due to disordered tonicity of muscle Akinisia-absence or poverty of movement |
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Atypical Antipsychotic
MOA: Binds to receptors in mesolimbic and mesocortical dopaminergic pathways– more selective than older drugs
Use: alleviates pos and neg symptoms
Adverse effects: hyperglycemia |
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atypical antipsychotic
Partial agonist activity at dopamine and serotonin 5-HT 1A receptors and antagonist activity at 5-HT2A receptors
Indicated for schizophrenia, bi-polar disorder, and depression |
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selective serotonin reuptake inhibitor |
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SSRI MOA: block serotonin reuptake transporter
indications: Indications include depression, bulimia, obsessive-compulsive disorder, social anxiety disorder, panic disorder, posttraumatic stress disorder
There’s bruxism and xerostomia. There may be some effects on platelet aggregation that would be exacerbated with aspirin and NSAIDs. No significant toxixity with overdose (advantage over TCAs) |
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Serotonin-Norepinephrine Reuptake Inhibitor Blocks both serotonin and norepi reuptake
Vasoconstrictor administered with caution May impair platelet aggregation Aspirin and NSAIDs |
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Serotonin-Norepinephrine Reuptake Inhibitor Blocks both serotonin and norepi reuptake
Indications: Depression and Neuropathic Pain
Dental adverse effect: Dry mouth Vasoconstrictor administered with caution May impair platelet aggregation Aspirin and NSAIDs |
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Serotonin-Norepinephrine Reuptake Inhibitor Block norepi and dopamine reuptake Weakly blocks serotonin reuptake
Indications: Depression, Nicotine Withdrawal
Dental adverse effect: Dry mouth Vasoconstrictor administered with caution May impair platelet aggregation Aspirin and NSAIDs |
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Serotonin antagonist/reuptake inhibitor (SARI) |
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Serotonin antagonist/reuptake inhibitor (SARI) |
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Used for depression that causes sleep disturbances
Orthostatic hypotension |
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Monoamine Oxidase Inhibitor |
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Mono amine oxidase inhibitors |
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For parkinsons prevent the degradation of dopamine to dopac. |
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catecholamine methyl transferase reduces the amount of dopamine by converting it to 3-methyoxytyramine. Inhibition will increase amount of dopamine. |
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Sinemet - Parkinsons
Unlabeled use of Sinemet is restless leg syndrome
Side effect: Abnormal involuntary movements of the orofacial muscles, Abnormal mouth movements, Protrusion and retraction of the tongue, Chewing motions, Facial grimacing
Oral problems: inflammation, damage to oral structures, movement of anterior teeth and difficulty wearing dentures. Dry mouth |
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Dopamine receptor agonist Potent D2,3 receptor agonist
Adverse effects include abnormal involuntary movements, confusion, psychosis and dry mouth
Compulsive behavior ?? Spending sprees, gambling |
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Dopamine receptor agonist Potent D3, 2, 4 receptor agonist
Adverse effects include abnormal involuntary movements, orthostatic hypertension, nausea, sedation/somnolence, dry mouth
Compulsive behavior ?? Spending sprees, gambling |
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Mechanism: NE and serotonin reuptake inhibitors
Also block muscarinic receptors and α1 adrenergic receptors
Adverse Effects: dry mouth, orthostatic hypotension
Indications: Depression, anxiety, obsessive-compulsive disorder (OCD)
IUSD Clinics-epi with TCA used “with restraint and caution” Drugs take 3 weeks to have an effect Overdose leads to cardiotoxicity--arrhythmias, MIs |
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GABAb receptor agoinist
Multiple Sclerosis Spinal cord injuries Patients who have had strokes
spasticity flexor spasms and concomitant pain muscular rigidity
Adverse Effect: sedation |
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Indications: Anxiolytic, sedative-hypnotic, amnesic, anticonvulsant, skeletal muscle relaxant, alcohol withdrawal
Inappropriate anxiety exists independently of a perceived threat and involves autonomic symptoms.
Examples: Generalized anxiety disorder Panic disorder Obsessive compulsive disorder Phobias
Adverse effects: Drowsiness, sedation, respiratory depression Psychological dependence—Schedule 4 Overdose does not cause death (wide therapeutic window) unless combined with other CNS depressant, usually alcohol Metabolized by CYP liver enzymes lots of drug interactions Erythromycin, clarithromycin and azole antifungals—inhibit hepatic metabolism of benzos |
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benzo Mechanism: Agonist at central benzo sites on the GABA receptor Drug of choice for sedation in pregnant women |
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benzo Interaction with GABA receptor close to benzo receptor Drug Interactions: not to be used with other benzodiazepines Ketoconazole, itraconazole, clarithromycin Lunesta |
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sodium channel inhibitors |
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Indications: Seizure disorders, bi-polar, neuralgias, migraines
Adverse effects: sedation |
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