Autonomic and Neuromuscular Pharm Flashcards
Selective MAO-B inhibitor that reduces the metabolism of dopamine. Used for the treatment of Parkinsonism.
Selegiline
A COMT inhibitor that is used with carbidopa/L-DOPA therapy in the treatment of Parkinsonism.
Tolcapone
Muscarinic cholinergic receptor agonists– Effects last longer than ACh, but have the same effect. Used in the treatment of GI and bladder… makes the GI tract and bladder contract more.. Can cause incontinence, diarrhea, and bradycardia
Bethanechol
Nicotinic cholinergic receptor agonist in the CNS; Used for cigarette withdrawal
Pilocarpine
Acetylcholinesterase inhibitor; ACh accumulates in synapse and produces a cholinergic response. Does NOT pass through BBB. Treatment for myasthenia gravis. Also used for GI and bladder paralysis, glaucoma, and treatment of anticholinergic effects produced by some drugs.
Neostigmine
________________ is an enzyme that breaks down ACh… these inhibitors help make the effect of the action last longer
acetylcholinesterase
Acetylcholinesterase inhibitors; ACh accumulates in synapse and produces a cholinergic response. Does pass through BBB. Commonly used to treat Alzheimer’s.
Donepazil
Muscarinic cholinergic receptor ANTAGONIST. Decreased PNS response. Blocks receptors from binding with ACh. Induces mydriasis (pupil dilation), reduces secretions (used pre-op), treatment of ventricular bradycardia, treatment of severe diarrhea and urinary incontinence.
Atropine
Muscarinic cholinergic receptor ANTAGONISTS. Decrease PNS response. Blocks receptors from binding with ACh.
Used in the treatment of motion sickness; inhibits cholinergic activation of the emesis center of the brain.
Scopolamine
Muscarinic cholinergic receptor ANTAGONISTS. Decrease PNS response. Blocks receptors from binding with ACh.
A M3 muscarinic cholinergic receptor antagonist that reduces PNS control over the contractile state of the urinary bladder muscle. It is helpful that it is selective to M3 receptors specifically because it wont cause other side effects such as eye problems and salivary problems.
Solifencacin
GABA receptor agonist that suppresses motor neuron activity and nerve conduction
Commonly used in patients with spinal cord injuries, treatment of spastic movement disorders
Baclofen
A nicotinic receptor antagonist on skeletal muscle; nondepolarizing relaxation because it blocks excitation-contraction coupling
Causes skeletal muscle relaxation, used during surgery, tracheal intubations and electro convulsant shock therapy
Pancuronium
Activates the ACh receptor and causes depolarization but it remains bound to the receptor for a prolonged period
Prolonged binding causes a conformational change in the shape of the receptor that leads to its inactivation, which then PREVENTS twitch summation and a sustained contraction (leading to relaxation).
Succinycholine
Inhibit membrane fusion proteins, necessary for exocytosis of ACh by motor neurons; blocks excitation-secretion coupling; this effect causes skeletal muscle paralysis
Block the secretion of ACh. Used for strabismus, overactive bladder, chronic migraines, botox in the face for wrinkles
Botulinum neurotoxins
Inhibits tyrosine hydroxylase, preventing the creation of L-Dopa in the cascade
Treatment for pheochromocytoma; tumor in the adrenal gland responsible for the excessive production of catecholamines and the development of severe htn
Methyltyrosine
Alpha 1 and 2 and beta 1 and 2 adrenergic receptor AGONIST which induces fight or flight
Used for eyedrops to dilate pupils for an exam, used as respiratory mists to induce bronchodilation in asthma pts, parenteral administration use for cardiac arrest and anaphylactic shock
epinephrine
AGONIST for D1, beta 1, and alpha 1 adrenergic receptors
Used to treat cardiogenic shock by acting as a renal D1 receptor agonist, mediating mesenteric blood vessel vasodilation to increase renal blood flow, preventing renal failure. Beta1 responses will increase cardiac output.
D1 = stimulated at low dose
Beta1 = stimulated at medium dose
Alpha1 = stimulated at high dose
Dopamine
Alpha1 receptor agonist. Can be used as a nasal decongestant which causes vasoconstriction of blood vessels in nasal mucosa… also used to treat prolonged responses to Viagra
Phenylephrine
Alpha1 receptor agonists
What is in Visine to help make eyes less red. Treat irritation of the eyes by vasoconstricting the blood vessels on the surface of the eye.
Tetrahydrozoline
Alpha2 receptor agonist that can pass through the blood brain barrier and reduce the release of catecholamines and SNS activity
Used as an antihypertensive drug.
Clonidine
Generalized beta1 and 2 receptor AGONIST
Cardiac stimulant used to treat cardiac arrest and heart failure
Isoproterenol
Selective beta1 AGONIST
Cardiac stimulant used to treat cardiac arrest and heart failure
Dobutamine
Selective beta2 AGONIST
Bronchodilator
Albuterol
Selective beta2 AGONIST
Reduce uterine contractions
Terbutaline
Selective beta3 AGONIST
Serves as an antispasmodic that is effective in the treatment of urinary incontinence and urgency
Mirabegron
Displaces catecholamines from internal stores, causing the release of NE
CNS stimulant that is used to treat narcolepsy, minimal brain disorders in the elderly and ADHD.
Amphetamine
Displaces NE from internal stores. Weak alpha1 and beta2 AGONIST
Can be used as a nasal decongestant and bronchodilator
ephedrine
Generalized alpha1 and 2 ANTAGONIST
Used in the treatment of frostbite, Raynauds. Increases blood flow to the skin. Can be used with extravasation in IVs to prevent necrosis.
Phentolamine
Selective alpha1 ANTAGONIST
Anti-hypertension agent; reduces peripheral vasoconstriction to renal and mesenteric vascular beds
Prazosin
Selective alpha1-a ANTAGONIST
Used to treat urinary tract obstruction in men with benign prostatic hyperplasia
Tamsulosin
Generalized beta1 and 2 receptor ANTAGONIST
Because its generalized, cannot be given to patients with asthma b/c it may cause bronchoconstriction.. Antihypertensive drug. Used for headaches/migraines
Propranolol
Selective beta1 receptor ANTAGONIST. Reduces cardiac output which activates carotid baroreceptos. Baroreceptors stimulate a SNS response that counter regulates the reduction in cardiac output.
Antihypertensive drug
Metoprolol
Both an alpha and beta ANTAGONIST. Reduces cardiac output (beta1 antagonism) and blocks compensatory vasomotor response by blocking alpha1 receptors in peripheral vascular system.
Antihypertensive drug
Labetalol
Beta1 antagonists used for managing blood pressure
propranolol and metoprolol
alpha1 antagonist used for managing blood pressure
prazosin
beta1 receptor antagonists decrease blood pressure by…?
reducing the secretion of renin in the RAAS system
beta receptor agonists are used after a patient has an MI because…
they reduce rhythm disorders
alpha 2 receptor agonist that decreases bp
clonidine
A drug that alters catacholamine synthesis
methyl-DOPA
Examples of catecholamines
epinephrine, norepinephrine, dopamine, isoproterenol, dobutamine
examples of noncatecholamines
phenylephrine, albuterol, and ephedrine
Which are less polar and more lipid soluble; catecholamines or noncatacholamines?
Noncatecholamines, making them able to pass through the BBB (phenylephrine, albuterol and ephedrine)
Why do catecholamines have a short half life?
Because of their metabolism by COMT and MAO
what enzyme is responsible for ach metabolism in the blood?
pseudocholinesterase
