drugs #1 8-18-15

Question 1

Metyrosine

Answer 1

Indication: Hypertension

MOA: Competitive inhibition of tyrosine hydroxylase

-rate limiting step in the production of catecholamines

Question 2

Reserpine

Answer 2

Indication: Hypertension

MOA: Inhibits VMAT uptake of monoamines

• VMATs transport monoamines into synaptic vesicles-keeps them from being degraded
• can cross BBB and lead to depression

Question 3

Bretylium

Answer 3

Indication: Ventricular Arrhythmia

MOA: Inhibit action potential generation and calcium dependent synaptic vesicle fusion

Question 4

Cocaine

Answer 4

Indication: Analgesia in surgery

MOA: Blocks monoamine reuptake

-re-uptake is the primary mode of terminating monoamines actions

Question 5

Amphetamine or Ephedrine

Answer 5

Indication: Narcolepsy, ADHD

MOA: Reverse monoamine reuptake transporters

Question 6

Naloxone, Naltrexone

Answer 6

Indication: Opioid overdose or dependence

MOA: Non- peptide blockers of opioid receptors in the CNS

Question 7

SSRI

Answer 7

Indication: Depression/Anxiety

MOA: Selective inhibition of serotonin reuptake transporter

Question 8

ACE inhibitors (eg. lisinopril)

Answer 8

Indication: Hypertension

MOA: Inhibit peptide cleavage of Angiotensin 1 to Angiotensin 2

Question 9

Phenylephrine

Answer 9

Indication: Hypotension during surgery

MOA: Direct agonist of adrenergic receptor

Question 10

MOA inhibitors

Answer 10

Indication: Depression

MOA: blockade of cytoplasmic metabolism of monoamines

Question 11

L-DOPA

Answer 11

Indication: Parkinson’s Disease

MOA: precursor of dopamine, stimulates dopamine production

Question 12

Carbidopa

Answer 12

Indication: Parkinson’s Disease

MOA: Blocks L-DOPA conversion to dopamine, does not cross BBB, so protects peripheral adrenergic neurons from producing too much dopamine and norepinephrine

Question 13

Tyramine

Answer 13

Indication: Ingested in diet, not therapeutic

MOA: competes with NE for transport into synaptic vesicle

• normally tyramine is subject to first pass metabolism by MAO in the liver
• when MOAs are inhibited such as treatment for depression-tyramine accumulates and is transported into adrenergic cells
• it competes with NE for transport into synaptic vesicles resulting in even higher levels of cytoplasmic NE than with MAO inhibitors alone
• reversal of uptake transporter
• excessive release of NE–>hypertensive crisis because of excessive vasoconstriction by NE in periphery
• newer drugs can selectively block MAO-a leaving MAO-B intact, allowing for tyramine degradation in the gut

Question 14

What are 6 indirect acting sympathomimetics?

Answer 14

1. amphetamine
2. methamphetamine
3. methylphenidate
4. ephedrine
5. pseudoephedrine
6. tyramine

Question 15

What are the PTIC for indirect acting sympathetics?

Answer 15

P:

1. Increased TPR and diastolic BP (a1+a2)
2. Positive ionotrophic and chronotropic effects, increased systolic pressure (B1)
3. CNS stimulant (probably increased NE)
4. Anorexia (probably increased DA)

T:
Tachycardia (b1)

I:
Attention Deficit Disorder
Narcolepsy
Nasal congestion

C:
Rx with MAO inhibitors within 2 weeks

Question 16

What are 3 Non-selective B-blockers?

Answer 16

1. Propranolol
2. Nadolol
3. Timolol

Question 17

Non-selective B-blockers

PTIC

Answer 17

P:
Decreased HR
Decreased contractility 
Decreased renin release 
Reduced sympathetic activation 
Inhibition of aqueous humor production 

T:
Bronchospasm
Mask symptoms of hypoglycemia
Bradycardia

I:
Hypertension
Angina
Glaucoma
Early to moderate heart failure
Arrhythmia
Thyrotoxicosis
Anxiety 

C:
Bronchospasm during asthma
Sinus bradycardia
2nd and 3rd degree heart block
cardiogenic shock

Question 18

What are 3 cardioselective B1 blockers?

Answer 18

metoprolol, atenolol, esmolol

Question 19

cardioselective B1-blockers

PTIC

Answer 19

P:
decreased HR
decreased contractility
decreased renin release
decreased sympathetic activation 

T:
hypotension
bradycardia

I:
hypertension
angina
arrhythmia

C:
sinus bradycardia
2nd and 3rd degree heart block
cardiogenic shock

Question 20

Pindolol

PTIC

Answer 20

partial agonist b-blocker
P:
decrease BP 
decrease contractility 
decrease renin release
decreased sympathetic activation 

T:
Hypotension

I:
Hypertension

C:
sinus bradycardia
2nd and 3rd degree heart block
cardiogenic shock

Question 21

What are two non-selective alpha blockers?

Answer 21

Phentolamine (reversible)

Phenoxybenzamine (irreversible)

Question 22

Non-selective alpha blockers?

PTIC

Answer 22

P: 
Decreased BP 
(alpha blockade +unmasks b effects)
Increased chronotropy and inotropy 
-->increased release of NE and reflex increase in NE release in response to hypotension 
-unmasks vasodilator effect of EPI 
(which has both alpha and beta effects)