Pharmocology Drug Summary Flashcards
Describe the classification, mechanism of action, and clinical uses of botulinum toxin
Classification: prevents release of acetylcholine
Mechanism of action: degrades SNARE & prevents vesicle fusion/ exocytosis
Clinical uses: paralyzes selected muscles with excessive tone
What are the major side effects of using botulinum toxin in a clinical setting?
Generalized muscle weakness or paralysis( depending on dosage, can be fatal)
What are the major considerations and contraindications of using botulinum toxins in a clinical setting?
Considerations: can reveal if patient has Lambert-Eaton syndrome… this disease will cause Botox to become generalized since release of ACh is still occurring
Contraindications: can be fatal if not localized
Describe the classification, mechanism of action, and clinical uses of neostigmine
Classsification: reversible anticholinesterase
Mechanism of action: carbamic acid derivative; longer duration of action; prevents ACh from being broken down by increasing 1/2 life of AChE
Clinical uses: used for treating Myasthania Gravis
What are the major side effects of neostigmine?
Bradychardia, diharrhea, salvation
What are the major considerations and contraindications of neostigmine?
Major considerations: increase of ACh in the synaptic cleft
Major contraindications: can depolarized too much & cause decrease of the effect
Describe the classification, mechanism of action, and clinical uses of physostigmine
Classification: reversible anticholinesterase
Mechanism of action: carbamic acid derivative; longer duration of action; prevents ACh from being broken down by increasing 1/2 life of AChE
Clinical uses: used for treating MG, crosses BBB good for CNS (GLUT 1 goes)
What is the major considerations of physostigmine ?
Used as treatment for atropine poisoning
What are the classifications, mechanism of action, and clinical uses of edrophonium?
Classification: reversible anticholinesterase
Mechanism of action: simple alcohol; short duration of action-increases ACh in cleft
Clinical uses- used for diagnosing Myasthenia Gravis (MG) and Eaton Lamburt
What are the major considerations of edrophonium?
Slight increase of ACh (for a little bit)
What are the classifications and mechanism of action of malathion?
Classification: irreversible anticholinesterase
Mechanism of action: phosphate group irreversibly binds to AChE, preventing ACh breakdown
What are the major side effects of malathion?
Increased ACh stimulates receptors causing muscle paralysis and death
What are the major considerations and contraindications of malathion?
Considerations- only way to overcome is with synthesis of new AChE which may take up to 6 weeks
Contraindications- Common way of suicide in African countries; irreversible toxic used in pesticides
What are the classifications, mechanism of action, and clinical uses of Succinylcholine?
Classification: neuromuscular nicotinic agonists “depolarizing”
Mechanism of action: keeps muscles from contracting by causing receptor channels to stay open, leading to depolarizing blockade
Clinical uses: used to produce paralysis of pharyngeal muscles for intubation & ventilation (short procedure)
What are the major side effects of Succinylcholine?
Bradychardia, K+ release (prolonged depolarozation), prolonged paralysis
What are the major therapeutic considerations and contraindications of Succinylcholine?
Considerations: leads to paralysis of the muscles due to desensitization to prolonged activation
Contraindications: can cause malignant hyperthermia
Uses parasympathetic
What are the classifications, mechanism of action and clinical uses of Pancuronium ?
Classification: neuromuscular nicotinic antagonists “nondepolarizing”
Mechanism of action: occupies the Nm receptors on skeletal muscle so agonist cannot bind and muscle cannot contract
Clinical uses: used to produce paralysis in surgery (long procedure)
What are the major side effects of Pancuronium?
Hypertension, apnea, bronchospasm, salivation & flushing
What are the major considerations and contraindications of Pancuronium?
Considerations- more selective on neuromuscular junction (Nm); long lasting- effects are overcom3 by increasing ACh levels
Contraindications- can cause respiratory failure
-sympathetic responses are dominating
What is the classification of acetylcholine?
Muscuranic agonist
What is the mechanism of action of acetylcholine?
Not used clinically
What is a major side effect of Acetylcholine ?
Too short half life
What are the major considerations and contraindications of acetylcholine?
Consideration: nicotinic & muscuranic agonists
Contraindications: too short half life
What are the classification, mechanism of action and clinical uses of pilocarpine?
Classification: muscuranic agonists
Mechanism of action: ACh is NOT used; mimics ACh effects
Clinical uses: used to treat glaucoma by activating receptors on circular muscles of eye causing miosis; used to treat dry mouth in Sjorgens syndrome
What are the major side effects of pilocarpine?
Stimulates parasympathetic
What are the major considerations and contraindications of pilocarpine?
Glaucoma & Sjorgen Syndrome treatment
What are the classifications, mechanisms, and clinical uses of methacholine?
Classification: muscuranic agonists
Mechanism of action : ACh is NOT used
Clinical uses: used in diagnosis of asthma (they will respond to lower dose)
What are the major side effects of methacholine?
Stimulates parasympathetic; bronchoconstriction
What are the major considerations and contraindications of methacholine?
Considerations: more specific for musculotenic because 3x more resistant to hydrolysis by AChE & possesses little affinity for nicotinic receptors
Contraindications: causes major bronchoconstriction
What are the classifications, clinical uses and mechanism of action of Bethanechol ?
Classification: muscuranic agonists
Mechanism of action: ACh is NOT used
Clinical uses: choose for promoting GI & urinary tract
What are the classifications, clinical uses and mechanism of action of Bethanechol ?
Classification: muscuranic agonists
Mechanism of action: ACh is NOT used
Clinical uses: choose for promoting GI & urinary tract
What is the major side effect of Bethanechol?
Stimulates parasympathetic
What are the major considerations of Bethanechol ?
Almost completely selective for muscuranic receptors
What are the classifications, clinical uses, and mechanism of action of atropine?
Classification: muscuranic antagonists
Mechanism of action: Bind to muscuranic receptor & prevents ACh from exerting its effect; blocks parasympathetic effects
Clinical uses: produce mydriasis (dilation of eyes), inhibit excessive salivation/ mucus secretion, counteract muscurine or anticholinesterase poisoning, & reverse sinus bradychardia
What are the major side effects of atropine?
Pupil dilation, tachycardia, decrease secretions, sympathetic response because antagonizes parasympathetic
What are the major considerations and contraindications of atropine?
Considerations: competitive antagonists; allows sympathetic response to dominate; reduces SLUDGE= salivation, lacrimation, urination, diaphoresis (sweating), GIT motility, Emesis
What are the cholinergic drugs?
- botulinum toxin
- neostigmine
- physostigmine
- edrophonium
- malathion
- suuccinylcholine
- Pancuronium
- pilocarpine
- methacholine
- Bethanechol
- atropine
What are the classifications, mechanism of action and clinical uses of amphetamine?
Classification: inhibitor of CA storage
Mechanism of action: Blocks NET
Clinical uses: displaces endogenous Catecholamine from storage vesicles
What is the major side effect of Bethanechol?
Stimulates parasympathetic
What are the major considerations of Bethanechol ?
Almost completely selective for muscuranic receptors
What are the classifications, clinical uses, and mechanism of action of atropine?
Classification: muscuranic antagonists
Mechanism of action: Bind to muscuranic receptor & prevents ACh from exerting its effect; blocks parasympathetic effects
Clinical uses: produce mydriasis (dilation of eyes), inhibit excessive salivation/ mucus secretion, counteract muscurine or anticholinesterase poisoning, & reverse sinus bradychardia
What are the major side effects of atropine?
Pupil dilation, tachycardia, decrease secretions, sympathetic response because antagonizes parasympathetic
What are the major considerations and contraindications of atropine?
Considerations: competitive antagonists; allows sympathetic response to dominate; reduces SLUDGE= salivation, lacrimation, urination, diaphoresis (sweating), GIT motility, Emesis
What are the cholinergic drugs?
- botulinum toxin
- neostigmine
- physostigmine
- edrophonium
- malathion
- suuccinylcholine
- Pancuronium
- pilocarpine
- methacholine
- Bethanechol
- atropine
What are the classifications, mechanism of action and clinical uses of amphetamine?
Classification: inhibitor of CA storage
Mechanism of action: Blocks NET
Clinical uses: displaces endogenous Catecholamine from storage vesicles
What are the major considerations of amphetamine?
Weak inhibitor of MAO
Alpha 1 is increased
What are the classifications, mechanism of action, and clinical uses of pseudoephedrine?
Classification: inhibitor of CA storage
Mechanism of action: increases NE activity at post synaptic a & B receptors
Clinical uses: used for nasal decongetion
What are the classifications, and mechanism of action of cocaine?
Classification: inhibitor of CA reuptake
Mechanism of action: inhibits NE Transporter
What are the classifications, mechanism of action and clinical uses of impramine?
Classification: inhibitor of CA reuptake
Mechanism of action: inhibitor of reuptake of Catecholamines
Clinical use: used for treating mild depression
What are the major side effects of impramine?
Post hypotension & tachycardia
What are the classifications, and mechanism of action of iproniazid?
Classification: inhibitor of CA metabolism
Mechanism of action: irreversible & non selective
What are the considerations and contraindications of ipromazid?
Considerations: would inhibit MAO or other things that degrade epinephrine & norepinephrine
Constipation : discontinued in most of the world besides France
What are the classifications, and clinical uses of epinephrine?
Classification: a & B agonist
Clinical use: at high doses, treats anaphylaxis & used for vasoconstriction in conjunction with local anaesthetics
What are the major considerations of using epinephrine?
High affinity for B2 receptors; at high concentration, has effect on a1
What are the classifications and considerations of norepinephrine?
Classification: a & B agonist
Considerations: high affinity for a1 & B1 but little affinity for B2
What are the classifications, mechanism of action and clinical uses of Oxymetazoline?
Classification: a1 & a2 agonist
Mechanism of action: vasoconstriction; a1 agonist & partial a2 agonist
Clinical use: decongestant
What is the considerations of oxymetazoline?
Topical or nasal; treats ocular hypermia- eye redness
Examples: vicks, Sudafed, afrin, visine
What is the classifications, mechanism of action and clinical use of phenylephrine?
Classification: a1 agonist
Mechanism of action: constriction & smooth muscle contraction
Clinical use: treatment of shock
What are the classifications, mechanism of action and clinical uses of Oxymetazoline?
Classification: a1 & a2 agonist
Mechanism of action: vasoconstriction; a1 agonist & partial a2 agonist
Clinical use: decongestant
What is the considerations of oxymetazoline?
Topical or nasal; treats ocular hypermia- eye redness
Examples: vicks, Sudafed, afrin, visine
What is the classifications, mechanism of action and clinical use of phenylephrine?
Classification: a1 agonist
Mechanism of action: constriction & smooth muscle contraction
Clinical use: treatment of shock
What are the classifications, mechanism of action and clinical uses of phenoxybenzamine?
Classification: a1 & a2 agonist
Mechanism of action: non-selective, non-competitive a-antagonist - irreversible
Clinical uses- Manage hypertension caused by pheochromocytoma- tumor of adrenal gland so NE is increased with this tumor
What is the major consideration of phenoxybenzamine?
Prevent vasoconstriction & decrease blood pressure
What are the classifications, mechanism of actions and clinical use of phentolamine?
Classification: a1 & a2 antagonist
Mechanism of action: reversible, competitive antagonists
Clinical uses: manage hypertension caused by pheochromocytoma
