Pharm Exam 1

Question 1

Name NE neurotranmission steps

a) START to vesicular release
b) synaptic cleft to END

Answer 1

1. Tyrosine through Na+ transporter
2. Tyrosine to Dopa [Tyrosine hydroxylase]
3. Dopa to Dopamine [Dopamine dopa decarboxylase]
4. Dopamine into vesicle [VMAT vesicular monoamine transporter)
5. Dopamine to NE [dopamine B hydroxylase]
6. AP => Ca2+ into cell
7. NE vesicle to surface and release into synaptic cleft
8. presynpatic (regulatory) receptor
9. postsynaptic (adrenergic) receptor
10. Diffusion
11. COMT (catechol-o-methyltransferase) break down
12. NET (NE tranporter) into presynpatic cytoplasm
    a) MOA (monoamine oxydase) metabolism
    b) VMAT transport back into vesicle (recycled)

Question 2

Catecholamine

Answer 2

Monoamine with catechole group (2 OH on aromatic ring)

1. DA
2. NE
3. Epi

Question 3

Monoamines

Answer 3

Amino group ---- aromatic ring by 2 carbon chain
Catecholamines and Seratonin
1. DA
2. NE
3. Epi
4. Seratonin

Question 4

Seratonin is a derivative of _____ while Catecholamines are a derivative of ______.

Answer 4

Tryptophan ——> Seratonin

Tyrosine —-> Catecholamines

Question 5

MOA and COMT are found where?
What problems could result?
Alternatives?

Answer 5

stomach
first pass effect
cannot be taken orally
*Non catecholamines Ephredrine and Ampethamine however can

Question 6

a1 receptor signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action?
Agonist treat?
Antagonist treat?

Answer 6

Gq

1. PLC activation
2. PLC converts DAG to PKC activation = protein phosphorylation
3. PLC converts IP3 to Ca2+ release from SR

Vasoconstriction in smooth muscle

Agonist

• decongestion
• tachycardia (SVT)

Antagonist

• HTN
• BPH
• Pheochromocytoma

Question 7

a2 receptor signal ______ pathway/protein. Which leads to ____, _____, and _____ within the pathway?

Action? (3)
Agonist treat? (3)

Answer 7

Gi

1. decrease cAMP
2. Ca2+ channels close in presynsaptic neuron
   - decrease neurotransmitter (vesicle) release
3. K+ channels open on postsynaptic neuron
   - hyperpolarize the postsynaptic neuron, harder to excite

decrease sympathetic output
inhibit insulin release (pancreatic B cells)
platelet aggregation (platelets)

Agonist

• HTN
• pain
• Glaucoma

Question 8

B1 receptor signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action? (3)
Agonist treat? (2)
Antagonist? (4)

Answer 8

Gs
activate adenylyl cyclase 
increase cAMP 
phosphorylation
-SR release Ca2+
-Ca2+ channels
-Troponin
=> contraction

Increase:
Force of contraction (inotropy)
HR (chrontropy)
speed up conduction in AV node
Kidney Renin release (incr BP)

Agonist

• shock
• CHF

Antagonist

• HTN
• Angina
• Arrhythmia
• CHF

Question 9

B2 receptor signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action? (3)
Agonist treat? (1)
Antagonist? (1)

Answer 9

Gs
activate adenylyl cyclase
increase cAMP
phosphorylation MLCK => relaxation

Relax smooth (bronchial) muscle
Increase plasma glucose from Liver
Vasodilate in skeletal muscle vasculature

Agonist

• Asthma
• premature labor

Antagonist
-Glaucoma

Question 10

B3 receptor signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action? (1)
Agonist treat? (1)

Answer 10

Gs
activate adenylyl cyclase
increase cAMP (phosphorylation)

Relax urinary bladder => prevent urination

Agonist
- overactive bladder

Question 11

Sympathetic system generally releases ____ postsynaptically but can also release what and to where?

Answer 11

NE
-smooth muscle and glands

ACh

• sweat glands
• muscarinic receptors

Dopamine

• to renal vessels
• Dopamine receptors

Epi
-adrenal medulla

Question 12

D1, D5 receptors signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action? (1)
Agonist treat? (1)

Answer 12

Gs
activate adenylyl cyclase
increase cAMP (phosphorylation)

dilate:
*renal vessels
mesenteric
cornary aa.

Agonist
- prevent kidney ischemia during Shock

Question 13

D2, D3, D4 receptors signal ______ pathway/protein. Which leads to ____ and _____ within the pathway?

Action? (1)
Agonist treat? (1)

Answer 13

Gi

1. decrease cAMP
2. Ca2+ channels close in presynsaptic neuron
   - decrease neurotransmitter (vesicle) release
3. K+ channels open on postsynaptic neuron
   - hyperpolarize the postsynaptic neuron, harder to excite

Question 14

Dopamine at low doses activates adrenergic receptors for _____ effects and at high doses _____.

Answer 14

low dose:
B1 on heart
D1 on renal, mesenteric, cornary vessels

high dose:
a1 vasoconstriction, incr BP