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Pharm > Pharm II > Flashcards

Pharm II Flashcards

1
Q

Epinephrine

A

Β>α,
low dose ↑ systolic ↓diastolic ↑CO
High dose α ↑BP vasoconstriction, ↑HR
-Bronchospasm β2 dilate, α1 ↓secretions

Use: Anaphylaxis, Cardiac arrest, bronchospasm

Toxicity: Arrhythmia

Contraindication: Late term pregnancy

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2
Q

Norepinephrine

A

α1, α2, β1:
vasoconstriction, ↑TPR ↑HR
β1↑systolic, α↑diastolic
*Baroreceptor reflex ↓HR from ↑↑BP

Use: Vasodilatory shock

Toxicity:
Ischemia
Arrhythmia
hypertension

Contraindication: Pre-existing vasoconstriction/ischemia,
late term pregnancy

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3
Q

Dopamine

A

D>β>α
Low dose D ↓TPR (at splanchnic vessels*)
Medium β1 ↑HR
Higher α ↑BP ↑TPR, vasoconstriction

Use: Hypotension due to low CO secondary to cardiogenic shock

Toxicity:
Low dose-hypotension
High dose-ischemia

Contraindication:
Uncorrected tachyarrhythmia or Ventricular Fibrillation

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4
Q

indirect sympathomimetics

Amphetamine
Methamphetamine
Methylphenidate
Ephedrine
Pseudophedrine
Thyramine
A 
Amphetamine
Methamphetamine
Methylphenidate
Ephedrine
Pseudophedrine
Thyramine
**A man mainly eats pizza toppings*

reverse reuptake channel- ↑ Ca independent release

Cardio: α vasocronstriction, ↑ diastolic; β ↑HR, contraction, ↑systolic ((May get baro ↓HR) balanced)

CNS: stimulant, anorexia agent
Toxicity: tachycardia
Use: ADD, narcolepsy, nasal congestion

Contraindication:Rx with MAO inhibitor 2wk, HTN

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5
Q

phenylephrine

A

α1 agonist-turns on α1

↑TPR ↑MAP ↓HR (baro reflex) Pupillary dilation
↓Broncho/sinus secretions

NOT at catecholamine

Use: SV tachycardia, Mydriatic, Nasal decongestant

Toxicity: Hypertension

Contra: Hypertension, Ventricular tachycardia

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6
Q

Clonidine

A

α2 agonist (recall α2 paired to Gαi- inhibit)

acute: ↑BP=periph, chronic: ↓BP=central
cross BBB, reduces sympathetic stimulation from pre-motor neuron: ↓constriction ↓BP by ↓SNS
periphery= minor vasoconstriction

Use: Hypertension due to SNS drive

Toxicity:
Dry mouth (↓secrete)
Bradycardia
Sedation

WITHDRAWL can be life-threatening hypertensive crisis

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7
Q

Non-selective β blocker

Propranolol
Nadolol
timolol

A 
Propranolol
Nadolol
timolol	
↓HR ↓contractiity ↓renin release (BP) 
↓SNS activation ↓aqueous humor (↓β)

Use: Hypertension, angina, glaucoma, early HF, arrhythmia

Contraindication:
Bronchospasm=asthma
Sinus bradycardia
2nd & 3rd Heart Block
Cardiogenic shock
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8
Q

Cardioselective

Atenolol
Metoprolol
Esmolol= Emergent

A

Atenolol
Metoprolol
Esmolol= Emergent (IV, small t1/2)

↓HR ↓contractiity ↓renin release (BP)
↓SNS activation

Use: Hypertension, angina, arrythmia Hypotension

Toxicity: Bradycardia
Dizzy, depressed, insomnia

Contraindication: Sinus bradycardia
2nd & 3rd Heart Block
Cardiogenic shock

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9
Q

Partial Agonist both B1 and B2

Pindolol

A

↓BP ↓contractiity ↓renin release (BP)
↓SNS activation

Use: Hypertension when other BB not tolerated

Toxicity: Bradycardia
Dizzy, depressed, insomnia

Contraindication: Sinus bradycardia
2nd & 3rd Heart Block
Cardiogenic shock

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10
Q

Phenoxybenzamine

A

Irreversible α antagonist-covalently binds

↓BP (block α allows β)
↑chronotrpy/ionotrpy

Use: Hypertension with pheochromocytoma (adrenal tumor),
Vasoconstrictor induced extravasation (iv)

Toxicity:
Prolonged hypotension
Reflex Tachycardia
Nasal congestion

Contraindication:
Coronary artery disease

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11
Q

Phentolamine

A

Irreversible α antagonist-covalently binds

↓BP (block α allows β)
↑chronotrpy/ionotrpy

Use: Hypertension with pheochromocytoma (adrenal tumor),
Vasoconstrictor induced extravasation (iv)

Toxicity:
Prolonged hypotension
Reflex Tachycardia
Nasal congestion

Contraindication:
Coronary artery disease

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12
Q

Selective α1 antagonist

A

Prazosin
Doxazosin
Terazosin
Please Don’t Touch

Inhinits vasoconstriction
Relax prostate sm

Use: Hypertension
Benign prostatic hyperplasia (BPH)

Toxicity:
Syncopy
Orthostatic Hypertension

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13
Q

Nicotine

A

Stimulate Nn in CNS,

Used in smoking cessation

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14
Q

Succinylcholine

A

Block Nm- nicotinic receptors @nm junction

Use: Blocks depolarization, blocks muscle contraction
Used as muscle relaxant for intubation/CST

Contraindication: FAMILIAL HYPERTHERMIA or skeletal muscle myopathy, recent crush injury

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15
Q

Quaternary Nitrogen Analog

A

Acetylcholine
Methacholine
Carbachol
Betanechol

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16
Q

Acetylcholine

A

Binds nicotinic and muscarinic, rapidly hydrolyzed by cholinesterase

No therapeutic use

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17
Q

Methacholine

A

Bind muscarinic on sm and heart

Hydrolyze more slowly, longer t1/2

Used to Dx bronchial hyperactivity (asthma) Bronchilar constriction

Contraindication: Pt on β-blocker, antidote is β- agonist (dilate bronchiole)

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18
Q

Carbachol

A

Muscarinic and nicotinic, resistant to acetylcholinesterase

Use: Opthalmo miotic (constrict) to ↓pressure in glaucoma or post Sx

Toxicity: Excessive muscarinic and nicotinic activation, only for topical use

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19
Q

Bethenchol

A

Muscarinic only, resistant to hydrolysis
GI tract and bladder ↑Nm input (M3)

Less M2 (heart activation)

Use: NON-Obstructive urinary retention (post partum/post-op)

Contraindication: Bradycardia Peptic ulcer, asthma, bradycardia

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20
Q

Naturally occurring tertiary ammines

A

Muscarine
No therapeutic use, resist hydrolysis

Pilocarpine
Pure muscarinic activity, CROSS BBB, on eye it contracts ciliary muscle & sphincter, flattening iris and allowing drainage of Aq. H.

Use:Dry mouth (radiation and Sjogrens Syn),
Treat glaucoma,

Contraindication: Careful with pt on β-blocker may slow HR (conduction)

21
Q

Cholinesterases

A

Acetylcholinesterase- synaptic cleft

Butyrylcholinesterase- plasma

22
Q

Neostigmine

A

Reversible cholinesterase inhibitor, skeletal muscle endplate

Tx myasthenia gravis, the loss of Nm receptor Reverse neuromuscular blockade

Toxicity: excess Ach action at peripheral Muscarinic and nicotinic receptors

Contraindication: Intestinal obstruction (M1)

23
Q

Endophonium

A

Inhibits cholinesterase reversibly, stimulates nicotinic receptors
(act fast and short)

Improve myasthenia gravis (not enough receptors, need more Ach), OR, worsen cholinergic crisis (too much Ach)

Use: Dx btwn Myasthenia gravis & Cholinergic crisis Toxicity: Bradycardia
Contraindication: Blocked intestinal or urinary tract

24
Q

Physostigmine

A

Cross BBB, slow hydrolysis by cholinesterase Use: Counteract delirium
Toxicity: Convulsions,
Contraindications: Asthma, cardiac insufficiency, GI blockage

25
Q

Donepezil

A

Treat Alzheimer’s, inhibits cholinesterase in CNS, long t1/2

26
Q

Organophosphate poisoning

A

Irreversible inhibitor cholinesterase

Diarrhea
Urination
Miosis
Bradycardia
Bronchorrea (secretions & constriction)
Emesis
Lacrimation
Salivation/Sweating
Gastrointestinal distress
Weakness/paralysis

Bumbbelss SLUDGE

Tx is atropine
Ventilation, suction, 2-PAM

27
Q

Echothiophate

A

Organophosphate, long-term miosis in glaucoma (topical)
Use: Glaucoma
Toxicity: Blurred vision, brow ache

28
Q

Muscarinic Antagonist

A

Atropine
Scopolamine
Glucopyrrolate

29
Q

Atropine

A 
Uses:
↓urgency urination
↓GI hypermobility
Tx cholinesterase inhibitor poisoning
Cause mydriasis/cycloplegia (optho)
Reverse bradycardia from vagal origin

Atropine Poisoning: Blind, Mad, Red, Hot, Dry, dilated, loss bowel and bladder tone, ↑HR and ↑BP

Tx toxicity with supportive measure, lower temp, catheter, kept in dark room, sedated

30
Q

Scopolamine

A

Sedative effect,
Use: Prepare for anesthesia and ↓secretions,
↓nausea and vomiting from chemo/motion sickness

Contraindication: Narrow angle glaucoma

31
Q

Glucopyrrolate

A

Used post-op, anti-muscarinic protects gut

32
Q

Curare drugs:
-non-depolarizing blocking drugs

Pancuronium
Tubocurarine
Vecuronium
Mivacurium
Rocuronium
A

Pancuronium :75 min
Tubocurarine 100 min- muscarinic block ↑HR↑CO
Vecuronium: 60 min
Mivacurium: 5 min** histamine release ↓BP
Rocuronium: 60 min- muscarinic block ↑HR↑CO

Note duration of action< t1/2
-Receptor Reserve: resp>course>fine>eye

NOT analgesic
Apnea (pt wont breathe)
-Inhaled anesthetic and antibiotics enhance effect

Antidote: cholinesterase inhibitors = neostigmine

Glucopyrrolate relieves effect on GI

33
Q

Succinylcholine

A

Depolarizing block, muscle depolarizes then gets stuck Fasciculation’s

  • Phase I is depolarized membrane (no antidote)
  • Phase II membrane repolarized but insensitive to Ach, Tx with cholinesterase inhibitor to ↑↑Ach

Rapid onset and metabolized in plasma, termination by diffusion away

Flaccid paralysis,

Intubation, ECT Cholinesterase inhibitors augment block (↑Ach↑depolarization)

Note:
non-analgesic, apnea, pt has pain from fascination, (arrhythmia, hypertension, bradycardia)
Hyper K+

Contraindication:
Malignant Hyperthermia and Muscle myopathy, recent trauma

34
Q

Spasmolytic: skeletal muscle relaxant

Baclofen
Tizanidine
Dantrolene
Benzodiazepines:
-diazepam, clonazepam	General idea
A
  • decease Ia fibers that excite the motor neuron
  • increase activity of inhibitory (GABA) internuncial neurons

net effect is decrease in motor neuron excitement

Tx for ↑sk. muscle tone

  • loss of supraspinal control
  • increase activation
  • increased α/γ motor stretch reflex
35
Q

Baclofen

A

GABA receptor agonist
-reduces Ca influx, reduces release excitate nt
*Cross BBB
Note- given orally or intrathecal catheter on spinal cord where needed

Tx: Spinal spasticity, MS Toxicity: Drowsiness

36
Q

Benzodiazepine

-diazepam, clonazepam

A

Facilitate GABA inhibition- allosteric on GABA receptor

↑likelihood of GABA binding its receptor, hyperpolarize membrane with Cl- (less likely to have an excitatory AP)

Use: Spinal spasticity, MS Toxicity: Drowsiness, sedation

37
Q

Tizanidine

A

α2 agonist (recall Gαi), less likely to have AP
- ↓PKA↓Pi on Ca channel, ↓AP thus opposes excitatory nt release

Use: Spinal spasticity, MS Toxicity: Drowsiness
Hypotension

38
Q

Dantrolene

A

Blocks Ca++ release from SR in skeletal muscle, “promotes weakness”
↓Ca↓ strength

Use: Spasticity, Malignant Hyperthermia

Toxicity: Muscle weakness, Sedation

39
Q

Metyrosine

A

Competitive inhibition of tyrosine hydroxylase (RL enzyme Tyr→ DOPA) Hypertension

40
Q

Reserpine

A

Blocks VMAT, dopamine does not get into vesicle Hypertension

41
Q

Bretylium

A

Hyperpolarizes membrane, stops AP and nt release Ventricular Arrhythmia

42
Q

Cocaine

A

Inhibits nt reuptake (dopamine, NE, SR) Analgesia in Sx (also a bad decision)

43
Q

Amphetamine

Ephedrine

A

Enters cell through monoamine reuptake (NE, Sr, Dopamine),
phosphorylates vesicular transporter & reuptake channel;↑cytosolic nt, and reverses channel ↑↑nt release non-ca dependent

Use: Narcolepsy, ADHD

44
Q

Naloxone

Naltrexone

A

Non-protein, cross BBB and block opioid receptor

Used in opioid overdose/dependence

45
Q

SSRIs

A

Does not allow SR reuptake from synapse Depression, anxiety

46
Q

ACE inhibitors, Lisinopril

A

Hypertension Inhibition of peptide cleavage Angio I to II (keeps it inactive)

47
Q

MAO inhibitors

A

MAO digests nt in cytosol from uptake, inhibition will ↑↑cytosolic nt, ↑nt released and may reverse reuptake channel direction allowing non Ca dependent nt release

Release WAY MORE nt

Use: depression

Toxic when taken with tyramine foods (rich, fermented)- competes with NE to get into vesicle

48
Q

L-DOPA

A

Precursor loading, ↑dopamine production

Use: Parkinson’s Disease

49
Q

Carbidopa

A

“eats up” dopamine in the periphery (does not cross BBB), allowing it to function in the CNS

Use: Parkinson’s Disease

Pharm (9 decks)

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