chap 6 continuation

Question 1

-adrenaline

-an agonist at both alpha and beta-receptors

-a very potent vasoconstrictor and cardiac stimulant (also inc. renin release)

Answer 1

Epinephrine

Question 2

-Levarterenol, noradrenaline (Levophed®)

-agonist at both alpha 1 and 2 receptors

-also has effect on beta 1 receptors but its effect on beta 2 receptors are not as much as epinephrine

Answer 2

NOREPINEPHRINE

Question 3

• the immediate precursor in the synthesis of NE
• important in sodium excretion and renal function
• an important neurotransmitter in the central nervous system and involved in the reward stimulus relevant to addiction
• Deficiency in ganglia: Parkinson’s Disease (Levodopa)
  Inc. level: Psychosis

Answer 3

Dopamine

Question 4

CV: activates β-receptors of the heart; very high doses stimulates α-receptors causing vasoconstriction

• Renal & visceral: dilates renal & splanchic arterioles resulting to increase blood flow to the kidneys and other viscera

Answer 4

dopamine

Question 5

• DOC for cardiogenic and septic shock
• Superior than NE because of increased blood flow in the kidneys
• Used to treat hypotension and severe heart failure

Answer 5

Dopamine

Question 6

• Isoprenaline, Isuprel®
  very potent B-receptor agonist and has little effect on alpha-receptors
• has positive inotropic and chronotropic actions; potent vasodilator

Answer 6

ISOPROTERENOL

Question 7

-a prodrug that is enzymatically hydrolyzed to desglymidodrine, a selective alpha-1 receptor agonist

-used for the treatment of orthostatic hypotension

Toxicity: Supine hypertension, piloerection, urinary retention

Answer 7

MIDODRINE

Question 8

-not a catecholamine, thus, not inactivated by COMT

-used to treat hypotension in hospitalized & surgical patients

-an effective mydriatic and decongestant and can be used to raise the blood pressure

Answer 8

PHENYLEPHRINE

Question 9

-acts like phenylephrine
may cause prolonged increase in blood pressure due to vasoconstriction

Answer 9

METHOXAMINE

Question 10

• Catapres®
  CA: Hypertension; Minimizes withdrawal symptoms accompanied in opiates, tobacco smoking & benzodiazepines
  S/E: dry mouth, sedation, lethargy, constipation, rebound hypertension

Answer 10

CLONIDINE

Question 11

indicated for sedation of initially intubated and mechanically ventilated partients during treatment in an intensive care setting; reduces requirement for opioids in pain control

Answer 11

Dexmedetomidine

Question 12

muscle relaxant

Answer 12

Tizanidine (Zanaflex®)

Question 13

• used in glaucoma to reduce IOP

Answer 13

Apraclonidine (Lopidine®) & Brimonidine (Alphagan®)

Question 14

used as topical decongestants because of their ability to promote constriction of the nasal mucosa; and relieves eye redness
- prolonged use may cause rebound congestion

Answer 14

Xylometazoline (Otrivin®)

Question 15

Dobutrex®
Effect: Positive inotropic effect
CA: Cardiogenic shock, Acute heart failure
Caution: can increase AV conduction in patients with atrial fibrillation; causes tolerance

Answer 15

DOBUTAMINE

Question 16

uterine relaxants
can be used in premature labor contraction

Answer 16

Terbutaline and Ritodrine

Question 17

-first orally active sympathomimetic drug
found in Ma Huang (Ephedra sinica)

-has the ability to activate beta-receptors – accounted for earlier use in asthma; used to treat hypotension
CNS: mild stimulant

Answer 17

EPHEDRINE

Question 18

Sudafed®
OTC as component of many decongestants
used as precursor in the illicit manufacture of methamphetamine

Answer 18

PSEUDOEPHEDRINE

Question 19

-common component of OTC appetite suppressants and nasal decongestants

-removed from the market because it was associated with hemorrhagic strokes in young women

Answer 19

PHENYLPROPANOLAMINE

Question 20

for Attention Deficit Hyperactivity Disorder (ADHD), and appetite suppression
- S/E: HTN, tachycardia, dependence, insomnia, seizures, psychosis

Answer 20

AMPHETAMINE

Question 21

very similar to amphetamine with an even higher ratio of central to peripheral actions

Answer 21

Methamphetamine

Question 22

a variant phenylisopropylamine with amphetamine-like effects; has been promoted as an anorexiant and a popular drug of abus

Answer 22

PHENMETRAZINE

Question 23

an amphetamine variant whose major pharmacologic effects and abuse potential are similar to those of amphetamine; may be effective in some children with attention deficit hyperactivity disorder

Answer 23

Methylphenidate

Question 24

-a psychostimulant that differs from amphetamine in structure, neurochemical profile, and behavioral effects

-MOA: inhibits both NE and Dopamine transporters, and increase interstitial concentrations of NE, dopamine, serotonin and glutamate while decreasing GABA levels

-used primarily to improve wakefulness in narcolepsy

Answer 24

modafinil

Question 25

-a normal by-product of tyrosine metabolism in the body and is also found in high concentrations in some fermented foods such as cheese -readily metabolized by MAO in the liver and is normally inactive when taken orally because of a very high first-pass effect -should not be taken with MAO inhibitors

Answer 25

Tyramine

Question 26

a selective inhibitor of NET used in the treatment of ADHD

Answer 26

Atomoxetine

Question 27

serotonin and NE reuptake inhibitor and is the only appetite suppressant approved by FDA for a long-term treatment of obesity

Answer 27

SIBUTRAMINE

Question 28

- a local anesthetic with a peripheral sympathomimetic action that results from inhibition of transmitter reuptake at noradrenergic synapses - readily enters CNS and produces an amphetamine-like psychological effect that is shorter lasting and more intense than amphetamine

Answer 28

COCAINE

Question 29

converted to dopamine in the body, and dopamine agonist with central actions are of considerable value in the treatment of Parkinson's disease

Answer 29

LEVODOPA

Question 30

is a D1-receptor agonist that selectively leads to peripheral vasodilation in some vascular beds; primary indication is in the intravenous treatment of severe hypertension

Answer 30

FENOLDOPAM