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Pharmacology > Autonomic Drugs > Flashcards

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
Q

Terbutaline

A

B2 agonists
Like albuterol but can be given subcutaneously
Treat acute bronchospasm and COPD
Delay premature labor

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25
Q

Ritodrine

A 
B2 agonist 
Uterine relaxant
IV administration
Stop premature labor 
May increase maternal morbidity
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26
Q

Salmeterol

A

B2 agonist
Aerosol inhalation
Long duration-not used for acute symptoms
Treats: asthma, bronchospasm, prophylaxis of exercise induced asthma, COPD
Toxicity: tremor and tachycardia

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27
Q

Caribidopa

A

Aromatic L amino acid decarboxylase
Inhibits metabolism of levodopa to dopamine in periphery but not CNS
Caribidopa plus levodopa treat Parkinson’s disease

29
Q

Edrophonium

A

Simple alcohol ACHe inhibitor
Reversibly binds
Acts only peripherally
Short duration of action-hydrogen bonds

30
Q

Neostigimine, pyridostigmine

A

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
Q

Physostigmine

A 
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
Q

Parathion and malathion (insecticides) so man and sarin (nerve gases)

A

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
Q

PBZ

A

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
Q

Phentolamine

A

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
Q

Prazosin

A

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
Q

Terazosin

A

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
Q

Doxasosin

A

Reversible A1 selective antagonist
Longer duration of action than terazosin
treats hypertension and BPH

38
Q

Tamsulosin

A

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
Q

Yonimbine

A

Alpha2 selective antagonist
treatment of orthostatic hypotension
reverse antihypertensive effects of an alpha2 agonist
side effects: tremor anxiety

40
Q

Propranolol

A

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
Q

Timolol

A

non selective beta blocker
Less lipid soluble than propanolol
no anesthetic effects
Treat hypertension, angina, migraine, open angle glaucoma

42
Q

Pindolol

A

Non selective beta blocker
Partial agonist of B1 and B2
less reduction in HR
Treat hypertensive patients with bradycardia and reduced cardiac reserve

43
Q

Atenolol

A 
B1 selective beta blocker
hydrophilic-no CNS
NO anesthetic or sympathomimetic activity
Treats: hypertension, angina, arrhytmias
Use with caution if patient has asthma
44
Q

Metoprolol

A 
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
Q

Esmolol

A

B1 selective beta blocker
Low lipid solubility
no anesthetic effects
Uses: emergency treatment of supraventricular tachycardia, arrhythmias associated with thyrotoxicosis, perioperative hypertension

46
Q

Labetalol

A 
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
Q

Carvedilol

A

Non selective B blocker and A1 blocker
no sympathomimetic activity
Vasodilation
Used: hypertension, congestive heart failure, myocardial ischemia

48
Q

Methacholine

A

Choline esters-direct muscaranic agonist
More resistant to hydrolysis than ACh
longer duration of action
Selective for cardiovascular receptors

49
Q

Betanechol

A

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
Q

Pilocarpine

A

Tertiary alkaloids selective for muscarinic receptors

induces sweat

51
Q

Nicotine

A

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
Q

Muscarine

A

Quarternary alkaloid selective for muscarnic receptors
From mushrooms
Causes sweat and salivary secretions

53
Q

Atropine

A

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
Q

Apraclonidine

A

Reduces IOP minimal systemic effects
Does not cross BBB
Short term

55
Q

Brimonidine

A

Reduces IOP with open angle glaucoma
Decreases aqueous humor production and increases outflow
Crosses BBB and causes hypotension And sedation

56
Q

Hexamethonium

A

Ganglionic blocker

Effective antihypersensitive

57
Q

Mecamylamine

A

Ganglionic blocker
Better absorbed via GI tract
Crosses BBB
Adjunct with nicotine patch

58
Q

Trimethapan

A

Short acting Ganglionic blocker
Given IV
Hypertensive emergencies

59
Q

Cisatracurium

A

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
Q

Vecuronium

A

Non depolarizing Nm blocker
Eliminated by liver and kidney
Most potent

61
Q

Mivacurium

A

Non depolarizing Nm blocker
Rapid onset and short duration of action
Metabolized by pseudocholinesterase

62
Q

Succinylcholine

A 
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
Q

Diazepam

A

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
Q

Baclofen

A

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
Q

Dantrolene

A

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
Q

Pralidoxime

A

ACHe inhibitor if given before aging occurs

67
Q

Tubocurarine

A

Non depolarizing antagonist at nicotinic receptor

68
Q

Cycloplegics

A

Paralyze ciliary muscle
Cyclopentonolate- muscarinic antagonist-longer duration
Tropicamide-muscarinic antagonist-short duration

Pharmacology (15 decks)

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