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PA 5250- Clinical Pharm > Neuropharm > Flashcards

Neuropharm Flashcards

1
Q

Cholinergic

A

refers to ACh

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2
Q

Preganglionic transmission of both divisions

A

ACh primary transmitter; acts on nicotinic receptors, causes release of epinephrine

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3
Q

Postganglionic parasympathetic fibers

A

ACH primary transmitter, acts on muscarinic receptors

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4
Q

Postganglionic Sympathetic fibers

A

Norepinephrine (NE) primary transmitter relased

Exception = ACh at sweat glands, dopamine in kidneys

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5
Q

Catecholamines

A

Norepi (NE)
Dopamine (DA)
Epinephrine (E)

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6
Q

Adrenergic

A

Refers to NE, E, DA

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7
Q

Catecholamine Synthesis

A 
Tyrosine
DOPA
Dopamine
Norepinephrine
Epinephrine
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8
Q

ACh in Cardiovascular system

A 
Vasodilation,
Negative chronotrope (rate)
Negative inotrope (force)
Negative domotrope (conduction velocity)
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9
Q

ACh in Respiratory tract

A

Bronchoconstriction
Increased secretion
Stimulation of carotid and aortic bodies

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10
Q

ACh in Urinary tract

A

Detrusor muscle contraction
Increased voiding pressure
Ureteral peristalsis

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11
Q

ACh in GI tract

A

Increased tone
Increased amplitude of contractions/peristalsis
Increased secretions in stomach and intestine

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12
Q

ACh additional effects

A

Miosis (pupil constriction)
Increased lacrimal, nasopharyngeal, salivary secretions
Increased production of sweat

Increased secretions all around!

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13
Q

SLUDGE

A 
Salivation
Lacrimation
Urination
Defecation
Gut pain/contraction
Emesis
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14
Q

BBM

A

Bronchospasm
Bronchorrhea (increased secretions in the bronchus)
Miosis

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15
Q

Muscarinic Agonists

A 
Ach
Methacholine
Carbachol
Bethanechol
Muscarine
Pilocarpine
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16
Q

Acetylcholine (Miochol-E)

A

Poor oral absorption

Used topically to produce miosis immediately after lens placement in cataract surgery

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17
Q

Methacholine (Provocholine)

A

Administered by inhalation to diagnose bronchial airway hyperactivity
Contraindicated in patients using beta-blockers (bb’s can induce some bronchoconstriction)
Onset 1-4 mins, duration 15-75

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18
Q

Bethanechol (Urecholine)

A

Treatment of urinary retention

Taken 3-4x daily on an empty stomach

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19
Q

Carbachol (Isopto Carbachol, Miostat)

A

Causes miosis during surgery

Reduces intraocular pressure in glaucoma

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20
Q

Pilocarpine (Salagen oral, Isopto Carpine opthalmic)

A

Non-selective muscarinic agonist (side effects with oral)
Treatment of xerostomia (dry mouth) due to radiation
Sjogren’s syndrome (decreased ability to produce salivation, lacrimation)

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21
Q

Cevimeline (Evoxac - oral)

A

More selective - high affinity ofr lacrimal and salivary muscarinic receptors
Less GI upset than pilocarpine

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22
Q

Muscarinic Agonists - Adverse Effects

A 
Sweating
Diarrhea, cramping
Nausea, vomiting
Sensation of tightness in bladder
Visual disturbances
Hypotension

Route of administration dictates side effects!!!!

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23
Q

Muscarinic Agonists - General Precautions

A
  • Asthma, COPD (bronchoconstriction)
  • Urinary obstruction
  • GI obstruction
  • Cardiovascular disease w/ hypotension, bradycardia
  • Hyperthyroidism
  • Acid-peptic disease
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24
Q

Muscarinic Antagonists

A

Bind muscarinic receptors and block Ach

Have little to no effect for nicotinic subtype

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25
Q

Atropine effects

A

Red as a beet, dry as a bone, blind as a bat, hot as a firestone, and mad as a hatter

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26
Q

Muscarinic Antagonist Cardiovascular effects

A

positive chronotropy (blood pressure unaffected)

Used for Vasovagal syncope and Asystole

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27
Q

Musc. Antagonist Respiratory effects

A

decreased bronchoconstriction
decreased secretions

Ipratropium, tiotropium (Spiriva)

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28
Q

Musc. Antagonist Eye effects

A

Mydriasis( dilation of pupils) long lasting

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29
Q

Musc. Antagonist GI tract effects

A

Antispasmodic, decrease acid secretion, decreased tone, amplitude and frequency of peristalsis

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30
Q

Musc. Antagonist other effects

A

Decreased salivation and nasal secretion.s

Decreased tone in urinary tract

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31
Q

Musc. Antagonists and CNS

A

Motion sickeness

Decrease extrapyramidal side effects of Parkinsons treatment

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32
Q

Musc. Antagonists and GU tract

A

For overactive bladder
Oxybutin - CYP3A4; lots of side effects
Tolterodine- more specific for bladder; CYP2D6
Trospium - only one eliminated significantly by kidneys

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33
Q

Muscarinic Antagonists Adverse Effects

A

Xerostomia
Constipation
Blurred vision
Cognitive impairment/feel fuzzy

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34
Q

Muscarinic Antagonists - Caution

A

Benign prostatic hyperplasia
GI obstruction
Urinary obstruction
Angle-closure glaucoma

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35
Q

Acetylcholinesterase Inhibitors

A

Also called anticholinesterases
Prevent breakdown of ACh
Increase ACh concentrations

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36
Q

Acetylcholinesterase Inhibitors - Therapeutic Uses

A
  • Atonic bladder and GI tract
  • Glaucoma
  • Reversal of neuromuscular blockade
  • Myasthenia gravis
  • Alzheimer’s disease (CNS issue)
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37
Q

Neostigmine

A

Relief of acute pseudo-colonic obstruction and/or post-op urinary retention

(Paralytic Ileus and Atony of the Urinary Bladder)

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38
Q

Anticholinesterase - Glaucoma

A

Contraction of ciliary muscle allows aqueous humor to flow out, decreasing intraocular pressure. Can be used, but not first choice.

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39
Q

Tensilon Test

A

To diagnose Myasthenia Gravis - an autoimmune neuromuscular disorder characterized by significant skeletal muscle weakness; appears to result in decrease in ACh receptors

40
Q

Myasthenia Gravis Treatment

A

Physostigmine q2-4h
Neostigmine q3-6h
Ambenonium q3-8h

Short acting drugs! have to be given constantly.

41
Q

Organophosphates

A

80% of pesticide-related hospitalizations
Responsible for over 200k deathers per year worldwide

SLUDGE will be apparent
Respiratory failure d/t hypersecreting

42
Q

Tx of Organophosphate Poisoning

A

Administer Atropine and pralidoxime STAT

Remove clothing, wash with soap and water, rinse eyes, maintain airway, do not induce vomiting!

43
Q

Sympathomimetic Actions

A
  1. Peripheral excitation on smooth muscle (skin, kidney, mucous membranes)
  2. Peripheral inhibition on smooth muscle (gut and bronchial)
  3. Cardiac excitiation
  4. Metabolic (glycogenolysis)
  5. Endocrine (renin, insulin, pituitary hormone)
  6. CNS (resp stimulation, increased psychomotor activity and wakefulness)
44
Q

Isoproteronol

A

A pure beta-agonist developed in 1940 with the benefit of no alpha activity. It is more potent than epinephrine at sites where both bind.

45
Q

Direct-acting Adrenergic Agonist

A

acts directly on adrenergic receptors (may be highly selective for their receptor; alpha or beta)

46
Q

Indirect-acting Adrenergic Agonist

A

availability of NE is increased via forcing the release of NE from storage vesicles or blocking uptake or metabolism

47
Q

Mixed-acting Adrenergic Agonists

A

Will share features of both direct and indirect; ephedrine works at receptor and also increases release of NE

48
Q

Therapeutic Uses of Sympathomimetics

A

Shock, hypotension, hypertension, arrhythmias, CHF, asthma, allergic rxns, opthalmic, narcolepsy, weight reduction, ADD/ADHD, local vascular and mucosal shrinkage

49
Q

Epinephrine - vascular effects

A

Potent Vasopressor
+ inotrope
+chronotrole
peripheral vasoconstriction

50
Q

Epinephrine - Cardiac effects

A

Used in cardiac arrest

  • direct B1 agonist
  • increased heart rate, cardiac output, O2 consumption
  • Cardiac efficiency decreases
51
Q

Epinephrine - Smooth muscle effects

A
  • Gut relaxation
  • Bladder sphincter contraction
  • Uterine contraction in non-preg, relaxation in near-term pregnancy
52
Q

Epinephrine - Respiratory effects

A
  • Strong B2 agonist
  • Bronchodilation
  • Useful in resp support of anaphylaxis, angioedema, asthma
53
Q

Epinephrine - Metabolic effects

A
  • predominant inhibition of insulin release
  • Increased glucose production (glucagon production and glycogenolysis)
  • breakdown of adipose tissue
54
Q

Epinephrine - Side efects

A 
Headache
Tremor
Palpitations
Restlessness
Cerebral hemorrhage (if bp too high)
Arrhythmias
55
Q

Norepinephrine - Cardiovascular effects

A

Strong periph vasoconstriction (due to no opposition from B2)
+Chronotrope
+inotropy in ventricles

Used for BP support in intensive care and shock - hospital only drug!

56
Q

Norepi receptors

A

slighly less potent than Epi at a receptors, equipotent at B1, and no appreciable effects at B2

57
Q

Norepi - Drug Interactions

A

MAOI
Antihistamines
Tricyclic antidepressants

58
Q

Norepi - Caution

A

Extremem hypertension may result

Extravasation (drug outside vein) can cause sloughing and necrosis

59
Q

Dopamine

A

Used in the management of shock. That’s it.

Only IV, does not cross BBB

60
Q

Dopamine - receptors

A

Dopamine receptors

B1 receptors

61
Q

Dopamine - Side effects

A

Increased sympathetic activity

Nausea, vomiting, headache

62
Q

Dopamine - Caution

A

Adjust dose if patient is taking MAOI

Beta-blockers interfere with cardiac effects

63
Q

Isoproteronol - receptors

A

Beta selective, no alpha activity

64
Q

Isoproteronol - Cardiovascular effects

A

Strong vasodilator
+inotrope
+chronotrope
+cardiac output

Used to treat some arrhythmias and bradycardia; largely been replaced

65
Q

Isoproteronol - side effects

A

headache, palpitations, flushing, tachycardia

66
Q

Dobutamine

A

Selective B1 agonist

67
Q

Dobutamine - Cardiovascular

A

Inotrope > Chronotrope
Increases output
Useful in cardiac decompensation after surgery and CHF

68
Q

Dobutamine Charge

A

CHF patient can receive infusion at hospital and have improved cardiac output for months

69
Q

Beta-2 Selective Agonists

A

In treatment of COPD and asthma, we want to minimize cardiac effects while producing bronchodilation

70
Q

Albuterol (Proventil, Proair, Ventolin)

A

SABA
Inhalation - dilation occurs w/in 15 mins, lasts 3-4h
Primary s/e = jittery or tachycardic

71
Q

Terbutaline

A

B2 selective agonist
Used via inhalation or IV for status asthmaticus
also used as tocolytic in preterm labor

72
Q

Long Acting Beta-2 Agonists (salmeterol, formoterol, advair)

A
  • Duration of action >12h
  • Tachyphylaxis is concern

you have an acute issue, use SABA, but already have LABA on board

73
Q

Alpha-1 selective adrenergic receptor agonists

A

Effects of these drugs are d/t activation of a adrenergic receptors in vascular smooth muscle
-blood pressure goes up or is maintained, so they are useful for patients with hypotension or shock

74
Q

Phelnylephrine

A
  • a-1 selective adrenergic receptor agonist
  • activates Beta receptors at high concentrations
  • when given IV, marked arterial vasoconstriction
  • also nasal decongestant and mydriatic
75
Q

Alpha-2 Selective Adrenergic Receptor

A

Used in treatment of hypertension - activates alpha-2 receptors in CNS which supress sympathetic activity

76
Q

Clonidine

A
  • a-2 selective
  • originally tested as a nasal decongestant, found to cause hypotension, sedation, and bradycardia
  • IV infusion causes opposite (rise in BP) than oral
77
Q

Apraclonidine

A
  • a-2 selective

- used topically to reduce intraocular pressure

78
Q

Bimonidine

A
  • a-2 selective
  • administered ocularly; lowers intraocular pressure
  • use in caution with patients w/ cardiovascular disease (slight hypotension, sedation can occur)
79
Q

Guanfacine

A
  • a-2 selective
  • More selective than Clonidine, works by same mechanism in brain stem
  • Approved by FDA to treat ADHD in children age 6-17
80
Q

Guanabenz

A
  • a-2 selective
  • Induces hypotension, sedation and bradycardia
  • dose adjust in liver patients
81
Q

Methyldopa

A
  • a-2 selective

- Metabolized by a-methylnorepinephrine in the brain which activates a-2 receptors and works similarly to clonidine

82
Q

Tizanidine

A
  • a-2 selective

- Muscle relaxant, treats spasticity related to cerebral and spinal disorders

83
Q

Amphetamine

A
  • Misc. sympathomimetic agonist
  • Schedule II - should only be used under medical supervision
  • powerful CNS stimulant and has peripheral a and B actions
84
Q

Amphetamine - Cardio

A

Raises both systolic and diastolic blood pressures.

Arrhythmias may occur in large doses

85
Q

Amphetamine - CNS

A
  • one of the most potent drugs for stimulating the CNS
  • Stimulates medullary respiratory center
  • lessens central depression caused by other drugs
86
Q

Amphetamine - Toxicity and Adverse Effects

A
  • CNS effects: restlessness, dizziness, tremor, hyperactive reflexes, talkativeness, tenseness, irritability, weakness, insomnia, fever and sometimes euphoria
  • headache, chills, pallor or flushing, palpitation, arrhythmias, angina, circulatory collapse, sweating, hyper or hypo tension
  • dry mouth, anorexia, N/V/D
87
Q

Amphetamine - Contraindications

A

Patients with anorexia, insomnia, asthenia, psychopathic personality, or a history of homicidal or suicidal tendencies

88
Q

Methamphetamine

A

Chemically closely related to amphetamines and ephedrine. Releases DA and other amines in the brain, inhibits MAO.

89
Q

Methylphenidate

A

Mild CNS stimulant; more mental than motor effects.

Large doses may lead to convulsions

90
Q

Ephedrine

A
  • Agonist of both alpha and beta receptors
  • Stimulates heart rate, CO, increase PVR => increases BP
  • increased resistance to urinary flow, bronchodilation, CNS stimulation
91
Q

Adrenergic Receptor Antagonists

A

Drugs that inhibit the interaction of NE, E and other drugs with alpha and beta receptors
- important for treatment of cardiovascular disease

92
Q

Alpha Adrenergic Receptor Antagonists

A

Alpha-1: contraction of arterial, venous and visceral smooth muscle
Alpha-2: suppression of sympathetic output, increasing vagal tone, facilitating platelet aggregation, inhibit release of NE and ACh from nerves, regulation of metabolic effects (suppression of insulin secretion and inhibition of lipolysis)

93
Q

Alpha-1 Receptor Antagonists

A

Blocking a-1 adrenergic receptors results in a fall of blood pressure; effects exaggerated if a-2 is blocked too

94
Q

Prazosin

A
  • alpha-1 receptor antagonist
  • used to treat hypertension (CHF and BPH also)
  • Adverse effects: hypotension and syncope
95
Q

Alpha-2 Receptor Antagonists

A

Increase sympathetic outflow, cause release of NE from nerve endings

PA 5250- Clinical Pharm (2 decks)

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