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Flashcards in Pharm2 6 Neuro pt1 Deck (35)
1

An action potential passing down an axon to the axon terminal changes the membrane potential resulting in ___ entry into the cell
This triggers the fusion of neuro-containing vesicles & cell membranes releasing neurochemical transmitters into the ____

Ca+2

synaptic cleft

2

What do Neurotransmitters (and the drugs that mimic them) do? (4)

block the uptake of neurotransmitters
block the re-uptake of neurotransmitters
enhance the release of neurotransmitters
enhance the uptake of neurotransmitters

3

as of yet, we cannot develop a drug that ...

BLOCKS the RELEASE of of a neurotransmitter

4

4 primary neurotransmitters

Norepinephrine (NE)
Acetylcholine (Ach)
Dopamine
Serotonin

5

A Lot of Different Things Can Occur near the Synapse (7)

Stop nerve impulse transmission to synapse
Stop precursor or neurotransmitter (NT) synthesis
Bind to or inactivate NT in cleft
Block NT post-synaptic receptor attachment
Inhibit re-release of precursor or NT
Inhibit reabsorption of precursor or NT
Inhibit re-synthesis of NT

6

Autonomic drugs are classified by

which receptor they act upon and either stimulate or block

7

4 types of Autonomic drugs (and what they do)

Sympathomimetics (adrenergic-agonists) stimulate the sympathetic nervous system (fight or flight)
Parasympathomimetics (cholinergic-agonists) produce the R&R response
Adrenergic-blockers inhibit sympathetic nervous system producing actions opposite to sympathomimetics
Anti-cholinergics (cholinergic-blockers) inhibit parasympathetic nervous system producing actions opposite to parasympathomemetics

8

Muscarinic Receptors
What's the NT, Primary locations, Responses

Acetylcholine (cholinergic)
Parasympathetic target; organs other than the heart
Stimulation of smooth muscle; gland secretions

9

Nicotinic Receptors
What's the NT, Primary locations, Responses

Acetylcholine (cholinergic)
Postganglionic neurons, skeletal muscle, neuromuscular junction
Stimulation of smooth muscle, gland secretions

10

Alpha1 Receptor
What's the NT, Primary locations, Responses

Norepinephrine (adrenergic)
All sympathetic target organs except the heart
Constrict blood vessels, dilate pupils

11

Alpha2 Receptor
What's the NT, Primary locations, Responses

Norepinephrine (adrenergic)
Pre-symaptic adrenergic nerve terminals
Inhibit release of norepinephrine

12

Beta1 Receptor
What's the NT, Primary locations, Responses

Norepinephrine (adrenergic)
Heart & kidneys
Increase HR, force of contraction; Renin release

13

Beta2 Receptor
What's the NT, Primary locations, Responses

Norepinephrine (adrenergic)
All sympathetic target organs except the heart
Inhibition of smooth muscle

14

What is the prototypical parasympathomimetic?

bethanechol

15

Prototypical Parasympathomimetic: bethanechol (Urecholine®)
Indication, MoA

Indications: Urinary retention
Mechanism of action: Direct acting parasympathomimetic, intefering with Ach receptors resulting in smooth muscle contraction, stimulating urinary & GI tracts

16

bethanechol (Urecholine®)
Adverse fx, CI

Adverse Effects: abdominal cramping, N&V, increased salivation, sweating, hypotension, syncope
Contraindications: Allergy, asthma, CAD, obstructive uropathy, bradycardia, BPH, hypotension, epilepsy, Parkinson’s, peptic ulcer, inflammatory GI disorders

17

What is the prototypical Anticholinergic?

Atropine sulfate

18

Atropine Sulfate (Atropine)
Indications
Mechanism of action

Indications: Bradycardia, facilitate ophthalmological exams, pre-anesthesia
Mechanism of action: Blocks Ach (muscarinic) receptors, induces symptoms of fight or flight, including increases heart rate, bronchodilation, decreases GI motility, mydriasis (pupilary dilation)

19

Atropine Sulfate (Atropine)
Adverse Effects
Contraindications

Adverse Effects: Tachycardia, palpitations, constipation and GI obstruction, may precipitate acute narrow angle glaucoma
Contraindications: Allergy, tachycardia, arrhythmias, CAD, history of bowel obstruction, history of glaucoma

20

What is the prototypical Sympathomimetic?

Albuterol Sulfate

21

Albuterol Sulfate (Proventil®)
Indications
Mechanism of action

Indications: Asthma, bronchospasm, reactive airway disease,
Mechanism of action: Selected Beta2-agonist, resulting in bronchial smooth muscle relaxation

22

Albuterol Sulfate (Proventil®)
Adverse Effects
Contraindications

Adverse Effects: Tachycardia, tremor, headache, hyperactivity, paradoxical bronchospasm, avoid with MAOIs, antagonized by beta-blockers
Contraindications: Allergy, arrhythmias, severe CAD/HTN

23

What is the prototypical beta Adrenergic-Blocker?

Metoprolol

24

metoprolol (Lopressor®)
Indications
Mechanism of action

Indications: Hypertension, tachyarrhythmias, AMI mortality reduction, AMI prophylaxis, angina prophylaxis
Mechanism of action: Inhibit the sympathetic nervous system, specifically by blocking beta-1 receptors primarily in the heart

25

metoprolol (Lopressor®)
Adverse Effects
Contraindications

Adverse Effects: Bradycardia, bronchospasm, fatigue, dizziness, depression, anhedonia, impotence
Contraindications: Severe bradycardia, 2nd/3rd degree heart block, overt CHF, cardiogenic shock, bronchospastic disease

26

What is the prototypical alpha Adrenergic blocker?

Doxazocin

27

Doxazocin (Cardura®)
Indications
Mechanism of action

Indications: Hypertension, BPH
Mechanism of action: Inhibit the sympathetic nervous system, specifically by selectively blocking alpha1 receptors primarily in vascular smooth muscle, dilating both arteries and veins as well as relaxing smooth muscle surrounding the prostate

28

Doxazocin (Cardura®)
Adverse Effects
Contraindications

Adverse Effects: Syncope, dizziness, orthostatic hypotension, esp. with first does and increasing doses
Contraindications: Allergy, hypotension,

29

How do SSRI's work?

Calcium fires to the end of a synapse, and NT in the synapse containing serotonin. The next nerve signals to send more Ca++

30

Why does Bethenechol worsen asthma?

Because of all the secretion of fluids (in mouth, lungs)

31

Why is CAD a contraindication for Bethanechol?

b/c they’ll be hypotensive and have coronary ischemia

32

What is obstructive uropathy (a CI for Bethanechol)

a kidney stone in their urethra

33

Why would you give Atropine in IV form? (2)

bradycardiia

tiny dose to dry up your mouth prior to anesthesia so you’re not choking on your own secretions.

34

Give a tiny dose of what to prevent a patient from choking on their own secretions while they are under anesthesia

Atropine sulfate

35

What is used to stop premature labor?

Albuterol sulfate