Autonomic Drugs Flashcards

0
Q

Vesamicol

A

Blocks VAT

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1
Q

Hemicholinium

A

Blocks CHT

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2
Q

Botulinum toxin

A

Cleaves SNARE proteins needed for vehicle fusion and exocytosis of ACh
Treats generalized spastic disorders and strabismus

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3
Q

Metyrosine

A

Blocks tyrosine hydroxylase

Treatment of inoperable pheochrmocytoma

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4
Q

Reserpine

A

Blocks VMAT

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5
Q

Cocaine

A

Blocks NET

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6
Q

Epinephrine

A

Released by adrenal medulla
Intramuscular injection
Contraction of arterioles, increased venous tone, cutaneous vasoconstriction, increased skeletal muscle flow
Stimulant, increased CO, increased O2 consum
Relax of GI smooth muscle, bronchodilation
Relief of hypersensitivity reactions, prolong anesthetics, hemostatic
Treatment of asthma
Adverse effects:headache anxiety fear, restlessness, palpitations

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7
Q

Norepinephrine

A

Increases total body resistance (less effect on B2)

Treat shock

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8
Q

Phenylephrine

A
Alpha 1 agonist
Maintain BP during anesthesia
Dilate eye (mydriatic)
Nasal decongestion
Not inactivated by COMT
Toxicity: rebound nasal congestion, headache, insomnia
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9
Q

Midodrine

A

A1 agonist
Hydrolyzed to desglymidodrine
Treats orthastatic hypertension with oral administration
Toxicity: supine hypertension, piloerecrion, urinary retention

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10
Q

Clonidine

A

Treatment of hypertension orally absorbed
Withdrawal from abused drugs
Inhibits adenylate cyclase
Increase BP then decrease sympathetic and BP
Adverse effects: dry mouth, sedation, sexual dysfunction

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11
Q

Isoproterenol

A

Beta agonist given parenterally or aerosol
Stimulates heart (1) vasodilator (2)
Increase CO Bronchodilation
Metabolized by liver- brief effect little clinical use
Adverse effects: palpitations, tachycardia, headache, flushing

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12
Q

Dopamine

A

Relatively selective B1
Low doses- increase renal flow, natriuresis, vomiting (D receptors)
Moderate doses: positive inotropy, release of NE
High doses: vasoconstriction
Parkinson’s disease
Used in severe congestive heart failure, cardiogenic shock,

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13
Q

Dobutamine

A

B1 agonist
Short duration-continuos IV administration
Drug of choice for cardiogenic shock

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14
Q

Albuterol

A

B2 agonist
Aerosol or orally administered short duration of action
Treat acute bronchospasm and COPD
Toxicity: tremor or tachycardia

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15
Q

Amphetamine

A

NET reuptake blocker
Increased alertness, decreased fatigue, appetite suppresant
Uses: narcolepsy and ADHD
Toxicity: headache, palpitations, tachyarrhythmias, excessive sweating, nausea, diarrhea

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16
Q

Ephedrine

A

Direct and indirect agonist
Ma huang-oral administration
Treats-chronic asthma, enuresis, nasal decongestion
CNS stimulant

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17
Q

Pseudoephedrine

A

Indirect release of NE
No B2 action
Nasal decongestant
Toxicity: atrial fibrillation, ventricular premature beats, hypertension, insomnia

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18
Q

Methylphenidate

A

Treats ADHD

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19
Q

Tyramine

A

Indirect agonist
By product of tyrosine metabolism
Metabolized by MAO-inactivated when orally administered
Hypertensive crisis occurs when people take MAO inhibitors

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20
Q

Cocaine

A

Inhibits dopamine reuptake and NE uptake inhibitor
Local anesthetic
Toxicity: cardiac arrhythmias, seizures, respiratory arrest, paranoia, tachycardia, hypertension, hyperthermia

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21
Q

Phenylzine

A

MAO-A and B inhibitor
A-increases NE, Epi, DA and serotonin
B-increases dopamine
Treats severe depression and Parkinson’s disease

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22
Q

Selegiline

A

MAO-B inhibitor
Increases dopamine
Treats severe depression and Parkinson’s disease

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23
Q

Entacapone

A

COMT inhibitor
Inhibits degradation of dopamine
Extends half life of levodopa
Treats Parkinson’s disease

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24
Terbutaline
B2 agonists Like albuterol but can be given subcutaneously Treat acute bronchospasm and COPD Delay premature labor
25
Ritodrine
``` B2 agonist Uterine relaxant IV administration Stop premature labor May increase maternal morbidity ```
26
Salmeterol
B2 agonist Aerosol inhalation Long duration-not used for acute symptoms Treats: asthma, bronchospasm, prophylaxis of exercise induced asthma, COPD Toxicity: tremor and tachycardia
27
Caribidopa
Aromatic L amino acid decarboxylase Inhibits metabolism of levodopa to dopamine in periphery but not CNS Caribidopa plus levodopa treat Parkinson's disease
29
Edrophonium
Simple alcohol ACHe inhibitor Reversibly binds Acts only peripherally Short duration of action-hydrogen bonds
30
Neostigimine, pyridostigmine
Carbamate inhibitors of ACHe Covalent bond-moderate duration of action CNS access limited Poor absorption from conjunctiva, skin, and lungs Neostigimine also minds nicotinic receptors
31
Physostigmine
``` Carbamate inhibitor of ACHe Covalent bond moderate length of action We'll absorbed by all routes of administration Gets access to CNS=toxic Used for anti cholinergic poisoning ```
32
Parathion and malathion (insecticides) so man and sarin (nerve gases)
Organophosphate ACHe inhibitors Hydrolyzed by ACHe resulting in stable enzyme complex Aging lengthens duration of action= irreversible (organophosphate-enzyme bond) Pralidoxime can be given before aging begins
33
PBZ
Irreversible non selective alpha antagonist Inhibits reuptake of NE Treats pheochromocytoma-adrenal medulla tumor Decreased peripheral resistance and BP Increase in CO and NE release, tachycardia Adverse effects: hypotension, myocardial ischemia, inability to ejaculate, dry mouth, fatigue, nausea, seizure
34
Phentolamine
Reversible non selective alpha antagonist Similar cardiovascular effects as PBZ Short term-BP control with phochromocytoma, treats hypertensive crisis, can help with erectile dysfunction Toxicity: hypotension, reflex tachycardia, abdominal pain, exacerbation of peptic ulcer
35
Prazosin
Reversible A1 selective antagonist Decreases peripheral vascular resisitance and venous return to heart Relaxes smooth muscle of prostate Decreases LDL and Triglyercides increases HDLs-hypertension treatment and symptomatic BPH Side effects: postural hypotension, and syncope
36
Terazosin
Reversible A1 selective antagonist More water soluble, higher bioavailability and longer duration of action than Prazosin Treatment for BPH and hypertension Side effect: postural hypotension and has shown to induce apoptosis in smooth muscle
37
Doxasosin
Reversible A1 selective antagonist Longer duration of action than terazosin treats hypertension and BPH
38
Tamsulosin
Competitive A1 antagonist Greater potency to prevent contraction of prostate than vascular smooth muscle Treat BPH Less likely to cause postural hypotension than other A1 antagonists Side effect: abnormal ejaculation
39
Yonimbine
Alpha2 selective antagonist treatment of orthostatic hypotension reverse antihypertensive effects of an alpha2 agonist side effects: tremor anxiety
40
Propranolol
Non selective beta blocker local anesthetic effects Lipophilic-oral administration-metabolized in liver Adverse effects: sedation and reduced libido Reduces HR and, Reduces renin Uses: hypertension, angina, arrhythmias, myocardial infarction, migraine
41
Timolol
non selective beta blocker Less lipid soluble than propanolol no anesthetic effects Treat hypertension, angina, migraine, open angle glaucoma
42
Pindolol
Non selective beta blocker Partial agonist of B1 and B2 less reduction in HR Treat hypertensive patients with bradycardia and reduced cardiac reserve
43
Atenolol
``` B1 selective beta blocker hydrophilic-no CNS NO anesthetic or sympathomimetic activity Treats: hypertension, angina, arrhytmias Use with caution if patient has asthma ```
44
Metoprolol
``` B1 selective beta blocker First pass effect No sympathomimetic activity Local anesthetic effects at high doses Treat: hypertension, mild heart failures, and arrhythmias Use with caution if patient has asthma ```
45
Esmolol
B1 selective beta blocker Low lipid solubility no anesthetic effects Uses: emergency treatment of supraventricular tachycardia, arrhythmias associated with thyrotoxicosis, perioperative hypertension
46
Labetalol
``` Non selective B blocker and A1 blocker B2 agonist Inhibits NE uptake First pass effect Vasodilation, loss of reflex-induced tachycardia Used for hypertension Hepatotoxicity ```
47
Carvedilol
Non selective B blocker and A1 blocker no sympathomimetic activity Vasodilation Used: hypertension, congestive heart failure, myocardial ischemia
48
Methacholine
Choline esters-direct muscaranic agonist More resistant to hydrolysis than ACh longer duration of action Selective for cardiovascular receptors
49
Betanechol
Choline esters-direct muscaranic agonist even more resistant to hydrolysis than ACh and Methacholine Stimulate GI tract, little effect on cardiovascular selectivity for bladder stimulation
50
Pilocarpine
Tertiary alkaloids selective for muscarinic receptors | induces sweat
51
Nicotine
tertiary alkaloid selective for nicotinic receptors stimulate and desensitize receptors increase respiratory rate, tremor, convulsions, vomiting Can cause hypertension, nausea, diarrhea, bladder voiding Used in insecticides
52
Muscarine
Quarternary alkaloid selective for muscarnic receptors From mushrooms Causes sweat and salivary secretions
53
Atropine
Binds to muscarinic receptor inhibits release of IP3 and inhibition of adenylyl cyclase Shifts equilibrium to inactive state Salivary, bronchial, and sweat glands Bradycardia, dry mouth loss of sweating
54
Apraclonidine
Reduces IOP minimal systemic effects Does not cross BBB Short term
55
Brimonidine
Reduces IOP with open angle glaucoma Decreases aqueous humor production and increases outflow Crosses BBB and causes hypotension And sedation
56
Hexamethonium
Ganglionic blocker | Effective antihypersensitive
57
Mecamylamine
Ganglionic blocker Better absorbed via GI tract Crosses BBB Adjunct with nicotine patch
58
Trimethapan
Short acting Ganglionic blocker Given IV Hypertensive emergencies
59
Cisatracurium
Nondepolarizing Nm receptor blocker Not dependent of renal or hepatic function Less likely to cause histamine release Prolonged relaxation for surgical procedures Mechanical ventilation in intensive care Prolonged apnea
60
Vecuronium
Non depolarizing Nm blocker Eliminated by liver and kidney Most potent
61
Mivacurium
Non depolarizing Nm blocker Rapid onset and short duration of action Metabolized by pseudocholinesterase
62
Succinylcholine
``` Depolarizing Nm blocker-muscle relaxant Agonist of nicotinic receptors IV short duration of action Desensitized end plate Rapid metabolism by pseudocholinesterase May increase IOP, deep muscle pain, ```
63
Diazepam
Spasmolytic drug GABA mediated chloride channel opening GABA AT GABA-A receptors Increases inhibition of primary afferents Enhances membrane hyper polarization Treat cerebral palsy, stroke, spinal cord injury, and muscle injury Oral or parental administration
64
Baclofen
Spasmolytic drug GABA-B agonist (mimetic) Hyper polarization by increased K+ conductance Spinal cord inhibition of a-motor neurons Intrathecal infusion Treat cerebral palsy, MS, and stroke
65
Dantrolene
Spasmolytic drug Inhibitor of Ca release from SR Binds to ryanodine receptor to prevent opening Oral administration Treats:SC injury, cerebral palsy, and MS and malignant hyperthermia Adverse effects: generalized muscle weakness sedation and hepatitis
66
Pralidoxime
ACHe inhibitor if given before aging occurs
67
Tubocurarine
Non depolarizing antagonist at nicotinic receptor
68
Cycloplegics
Paralyze ciliary muscle Cyclopentonolate- muscarinic antagonist-longer duration Tropicamide-muscarinic antagonist-short duration