Term
Neuromuscular blocking agents
MOA |
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Definition
Block acetylcholine from activating nicotinicM receptors on skeletal muscles
Cause muscle relaxation |
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Term
Neuromuscular blocking agents
Uses |
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Definition
Surgery for muscle relaxation
Endotracheal intubation
Mechanical ventilation
Other diagnostic procedures |
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Term
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Definition
Nondepolarizing Neuromuscular Blockers II
Intermediate-acting agents – duration 20-40 min. |
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Term
| Succinylcholine (Anectine) |
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Definition
Mechanism of action –Binds to Nicotinic – M receptors on the motor end plate of muscle.
Pharmacologic effects
Muscle relaxation – flaccid paralysis
Central nervous system- no effect
Pharmacokinetics – peak 1min, duration 4-10 min. Ultra short acting drug.
Therapeutic uses- EET
Adverse effects
Prolonged apnea in patients with low pseudocholinesterase activity
Malignant hyperthermia
Postoperative muscle pain – neck & shoulders
Hyperkalemia
Drug interactions
Cholinesterase inhibitors – potentiate effects
Antibiotics- intensify effects
Toxicology
Preparations, dosage, and administration – 25-75mg IV |
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Term
| Therapeutic Uses of Neuromuscular Blockers |
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Definition
Muscle relaxation during surgery
Facilitation of mechanical ventilation
Adjunct to electroconvulsive therapy
Endotracheal intubation
Diagnosis of myasthenia gravis |
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Term
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Definition
Nondepolarizing Neuromuscular Blockers II
Intermediate-acting agents – duration 20-40 min. |
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Term
| Therapeutic Applications of Alpha1 Activation |
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Definition
Hemostasis (vasoconstriction)
Nasal decongestion
Adjunct to local anesthesia – delays anesthesia absorption
Elevation of blood pressure (vasoconstriction)
Mydriasis (dilatation of pupil) |
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Term
| Adverse Effects of Alpha1 Activation |
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Definition
Hypertension
Necrosis
Bradycardia |
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Term
| Therapeutic Application of Beta1 Activation |
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Definition
Cardiac arrest
Heart failure
Shock
AV heart block |
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Term
| Adverse Effects of Beta1 Activation |
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Definition
Altered heart rate or rhythm
Angina pectoris |
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Term
| Therapeutic applications of beta2 activation |
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Definition
Asthma – terbutaline inhalation
Delay of preterm labor |
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Term
| Adverse Effects of Beta2 Activation |
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Definition
Hyperglycemia – only in DM
Tremor – most common due to skeletal muscle contractions |
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Term
| Clinical Consequences of Dopamine Receptor Activation |
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Definition
Activation of peripheral dopamine receptors causes dilation of the vasculature of the kidneys.
Dopamine is only drug to activate dopamine receptors |
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Term
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Definition
Receptor specificity - alpha1, alpha2, beta1, beta2.
Therapeutic uses- pg. 157
Adverse effects
Hypertensive crisis – alpha 1
Dysrhythmias – beta 1
Angina pectoris – beta 1
Necrosis following extravasation
Hyperglycemia – beta 2 in DM
Drug interactions
MAO inhibitors
Tricyclic antidepressants
General anesthetics
Alpha-adrenergic blocking agents
Beta-adrenergic blocking agents
Preparations, dosage, and administration – any route |
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Term
| Norepinephrine (Levophed) |
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Definition
Receptor specificity
Alpha1,Alpha2, Beta1
Chemical classification
Catecholamine
Adverse effects
Hypertensive crisis – alpha 1
Dysrhythmias – beta 1
Angina pectoris – beta 1
Necrosis following extravasation
**Clinical applications = hypotensive states & cardiac arrest. IV ONLY |
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Term
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Definition
Receptor specificity: beta1 and beta2
Chemical classification: catecholamine
Therapeutic uses
Cardiovascular – AV block, Inc. cardiac output, shock.
Asthma – bronchodilation although has been abandoned due to cardiac effects.
Bronchospasm
Adverse effects – tachydysrhythmias, angina pectoris, hyperglycemia.
Drug interactions- MAO Inhibitors
Preparations and administration – 0.2-0.02 mg/ml |
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Term
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Definition
Receptor specificity: dopamine, beta1, (high doses) alpha1
Therapeutic uses
Shock
Heart failure
Acute renal failure ???
Adverse effects – tachycardia, dysrhythmias, & anginal pain
Drug interactions - MAO Inhibitors
Preparations, dosage, and administration
Preparations: is dispensed in aqueous solutions
Dosage: must be diluted
Administration: administered by IV, 2-5 mcg/kg/min |
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Term
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Definition
Receptor specificity: beta1
Chemical classification: catecholamine
Actions and uses – heart failure
Adverse effects – Tachycardia, monitor BP and ECG.
Drug interactions - MAO Inhibitors
Preparations, dosage, and administration
Preparations: is dispensed in aqueous solutions
Dosage: must be diluted
Administration: administered by IV, 2.5 - 10 mcg/kg/min |
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Term
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Definition
Receptor specificity: beta2
Chemical classification: noncatecholamine
Therapeutic uses
Asthma
Delay of preterm labor
Adverse effects
Tremor & Tachycardia
Minimal at therapeutic doses |
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Term
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Definition
| Direct blockade of adrenergic receptors |
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Term
Alpha-adrenergic blocking agent
Uses |
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Definition
Therapeutic
Essential hypertension
Benign prostatic hyperplasia hyperplasia (BPH) (decrease contraction of smooth muscle in bladder)
Raynaud’s disease – peripheral vascular disorder with vasospasms in the toes and fingers.
Overdose of alpha1 agonist |
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Term
| Alpha-adrenergic blocking agent |
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Definition
Nonselective
Produces alpha1 and alpha2 blockade
Selective
Produces alpha1 blockade |
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Term
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Definition
Alpha-Adrenergic Blocking Agents
Selective
Produces alpha1 blockade
Actions and uses – dilation of arterioles & veins, relaxation of smooth muscles & prostatic capsule.
Pharmacokinetics – peak 1-3 hours, duration 10 hours.
Adverse effects – Orthostatic hypotension, reflex tachycardia.
Preparations, dosage, and administration – (1,2, & 5 mg tabs) Adult dose 1mg bid. |
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Term
Alpha-1 Blockade
Adverse Effects |
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Definition
Orthostatic hypotension
Reflex tachycardia
Nasal congestion
Inhibition of ejaculation – sexual dysfunction (nonadherence)
Sodium retention and increased blood volume – may see lasix in conjunction with this type of med. |
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Term
Orthostatic hypotension
Reflex tachycardia
Nasal congestion
Inhibition of ejaculation – sexual dysfunction (nonadherence)
Sodium retention and increased blood volume – may see lasix in conjunction with this type of med. |
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Definition
| The most significant adverse effect associated with alpha2 blockade is potentiation of the reflex tachycardia. |
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Term
| Beta-Adrenergic Blocking Agents |
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Definition
Nonselective
Blocks beta1 and beta2 receptors
Cardioselective
Blocks beta1 receptors |
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Term
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Definition
Cardioselective
blocks beta 1
Pharmacologic effects - dec. HR& dec. CO. but does not block bronchial beta 2 receptors.
Pharmacokinetics – lipid soluble
Therapeutic uses - HTN
Adverse effects – Bradycardia, AV heart block, Heart failure, Rebound cardiac excitation
Precautions, warnings, and contraindications – Sinus brady, heart failure. Safer with asthma & DM
Preparations, dosage, and administration – 50-100mg QD. |
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Term
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Definition
Nonselective
beta 1 & beta 2
Pharmacologic effects – dec. HR& dec. CO
Pharmacokinetics – highly lipid soluble
Therapeutic uses – HTN, angina, MI
Adverse effects
Bradycardia
AV heart block
Heart failure
Rebound cardiac excitation
Bronchoconstriction
Inhibition of glycogenolysis
CNS effects – derpession, insomnia, nightmares, & hallucinations
Precautions, warnings, and contraindications
Severe allergy – avoid
Diabetes – masks hypoglycemia and Tachycardia (defense mechanism)
Cardiac, respiratory, and psychiatric disorders
Drug interactions
Calcium channel blockers – same effects
Insulin
Preparations, dosage, and administration
General dosing considerations
Preparations – (10-90 mg)
Dosage – (40 mg BID) |
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Term
| Beta-Adrenergic Antagonists I: Therapeutic Responses to Beta Blockade |
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Definition
(reduced heart rate, reduced force of contraction, & reduced velocity of impulse)
Therapeutic applications of beta blockade:
Angina pectoris – decrease cardiac work.
Hypertension & Cardiac dysrhythmias – reduce PVR.
Myocardial infarction – reduces pain and infarct size
Heart failure
Hyperthyroidism
Migraine
Stage fright
Pheochromocytoma – large amt. of catecholamines
Glaucoma |
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Term
| Beta-Adrenergic Antagonists I: Adverse Responses to Beta Blockade |
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Definition
Adverse effects of beta blockade involve both beta1 and beta2 blockade.
Adverse effects of beta1 blockade: most common
Bradycardia
Reduced cardiac output –use with caution in heart failure
Precipitation of heart failure
AV heart block
Rebound cardiac excitation – do not stop abruptly!
Adverse effects of beta2 blockade:
Bronchoconstriction – contraindicated with Asthma.
Inhibition of glycogenolysis – may cause hypoglycemia |
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Term
Parasympathetic Nervous System (PSNS)
The regulatory functions of PNS affect these sites |
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Definition
Heart rate- slows down
Gastric secretions - Increased
Bladder and bowel - Empties
Vision – focuses the eyes for near vision (constricts pupil)
Bronchial smooth muscle - contracted |
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Term
| Parasympathetic Nervous System (PSNS) |
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Definition
| Conserves Energy (by releasing the cholinergic neurohormone acetylcholine) |
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Term
| Sympathetic Nervous System |
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Definition
| Controls energy expenditure in stressful situations by releasing the adrenergic catecholamine norepinephrine |
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Term
| Main functions of the Sympathetic Nervous System |
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Definition
Regulation of cardiovascular system
Regulation of body temperature
Implementation of “fight or flight” reaction |
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Term
| Neurotransmitters of the Peripheral Nervous System (PNS) |
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Definition
Acetylcholine
Norepinephrine
Epinephrine
Dopamine |
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Term
| Cholinergic receptor mediated by ? |
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Definition
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Term
| Adrenergic receptors mediated by? |
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Definition
| norepinephrine and epinephrine |
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Term
| Dopamine Receptor mediated by? |
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Definition
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Term
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Definition
A molecular structure within a cell or on the surface characterized by:
Selective binding of a specific substance
Specific physiologic effect that accompanies the binding (like neurotransmitters) |
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Term
| Adrenergic Receptor (Alpha and Beta) |
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Definition
| Sites on effector organs innervated by postganglionic adrenergic fibers of the SNS, classified as Alpha and Beta adrenergic receptors according to their reaction to norepinephrine and epinephrine, respectively, and to certain blocking and stimulating agents |
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Term
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Definition
Adrenergic receptors that respond particularly to epinephrine and to such blocking agents as propanolol.
Subdivided into Beta 1 and Beta 2, and Beta 3 (atypical) |
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Term
| Cholinergic Receptor (Muscarinic and Nicotinic) |
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Definition
| Cell-surface receptors that bind the neurotransmitter acetylcholine and mediate its action on postjunctional cells, including parasympathetic autonomic effector cells, sympathetic and parasympathetic autonomic ganglion cells, striated muscle, and certain central neurons |
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Term
| Subtypes of Cholinergic receptors |
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Definition
Nicotinic n
Nicotinic m
Muscarinic |
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Term
| Subtypes of adrenergic receptors |
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Definition
Alpha1 and alpha2
Beta1 and beta2
Dopamine |
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Term
| Nicotinic n (neuronal)receptor function |
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Definition
Promotes ganglia transmission
Promotes release of epinephrine |
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Term
| Nicotinic m (muscle) receptor function |
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Definition
| Contraction of skeletal muscle |
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Term
| Muscarinic receptor function |
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Definition
| Activates parasympathetic nervous system |
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Term
Alpha1 receptor function
(adrenergic) |
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Definition
Vasoconstriction
Ejaculation
Contraction of bladder neck and prostate |
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Term
Alpha2 receptor function
(adrenergic) |
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Definition
Located in presynaptic junction
Minimal clinical significance
Mediator of Negative Feedback preventing further release of Nor-epi |
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Term
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Definition
Bronchial dilation
Relaxation of uterine muscle
Vasodilation
Glycogenolysis (Inc. Blood sugar in DM) |
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Term
| Dopamine receptor function |
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Definition
| Dilates renal blood vessels |
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Term
| Epinephrine receptor specificity |
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Definition
| can activate all alpha and beta receptors, but not dopamine receptors |
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Term
| Norepinephrine specificity |
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Definition
| can activate alpha1, apha2, and beta1, receptors, but not beta2 or dopamine receptors. |
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Term
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Definition
can activate alpha1, beta1, and dopamine receptors.
Dopamine is the only neurotransmitter capable of activating dopamine receptors. |
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Term
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Definition
| A drug that has an affinity for and stimulates physiologic activity at cell receptors normally stimulated by naturally occurring substances |
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Term
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Definition
| A substance that tends to nullify the action of another, as a drug that binds to a cell receptor without eliciting a biological response, blocking binding of substances that could elicit such responses |
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Term
Muscarinic Antagonist
(Anticholinergic/parasympatholytic) |
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Definition
Drug that blocks the action of acetylcholine at muscarinic receptors
e.g. atropine |
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Term
Muscarinic Antagonist (Atropine)
Characteristics |
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Definition
Actions
Increases heart rate
Decreases secretions
Relaxes bronchi
Decreases bladder tone
Decreases GI tone and motility
Dilates the pupil
CNS excitation
Uses
– Preanesthestic
Disorders of the eye
Bradycardia
Intestinal hypertoxicity and hypermotility
Muscarinic agonist poisoning
Asthma
– Biliary colic
Peptic ulcer disease
Adverse effects
Dry mouth (xerostomia)
Blurred vision
Photophobia
Increased intraocular pressure
Urinary retention
Constipation
Tachycardia
– Anhydrosis
– Asthma
Drug interactions
Avoid combining atropine with other drugs capable of causing muscarinic blockade. (antihistamines, antipsychotics, & tricyclic antidepressants)
Preparations, dosage, and administration
0.4 mg tab or 0.05-1mg/ml. Average adult dose = 0.5mg |
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Term
| Muscarinic Agonists (Parasympathomimetic) |
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Definition
Uses
Urinary retention
GERD
Ileus
Postoperative abdominal distention
Glaucoma
Adverse effects
Exacerbation of asthma |
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