IPS2: Pharmacology - Part 2.2.1 - Autonomic Drugs - Sympathetic drugs Part 1 - Introduction, Sympathomimetics

Natural catecholamines except:

a. Posses catechol nucleus

b. Posses ethylamine side chains

c. Include Epinephrine, Norepinephrine, and Dopamine.

d. Endogenous

e. All

f. None

f. None

Catechol nucleus:

a. Benzene ring

b. With 2 OH group at para position

c. With 2 OH group at ortho position

d. a and b

e. a and c

e. a and c

Biosynthesis of natural catecholamines except:

a. Amino acid precursor is glycine.

b. Tyrosine hydroxylase is the first enzyme needed thus the rate limiting step.

c. Dopamine is the first catecholamine synthesized.

d. Epinephrine is the last catecholamine synthesized.

e. None

a. Amino acid precursor is glycine.

Biosynthesis of natural catecholamines:

a) Amino acid precursor is TYROSINE.

b) Tyrosine hydroxylase is the first enzyme needed thus the rate limiting step.

c) Dopamine is the first catecholamine synthesized.

d) Epinephrine is the last catecholamine synthesized.

Convert tyrosine to dopa.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

a. Tryosine hydroxylase

Convert dopa to dopamine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

b. Dopa decarboxylase

Convert dopamine to norepinephrine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

c. Dopamine B-hydroxylase

Convert norpepinephrine to epinephrine.

a. Tryosine hydroxylase

b. Dopa decarboxylase

c. Dopamine B-hydroxylase

d. 2PNMT

e. Epinephrine

d. 2PNMT

Norepinephrine:

a. A fraction can reach the adrenal medulla

b. 2PNMT is present in the adrenal medulla

c. 2PNMT convert norepinephrine in the adrenal medulla synthesizing epinephrine.

d. a and b

e. b and c

f. All

f. All

Adrenal gland:

a. Gland superior to kidney

b. Cortex is the outer layer (Adrenal cortex)

c. Medulla is the inner layer (Adrenal medulla)

d. a and b

e. b and c

f. All

f. All

Mechanism of storage of neurotransmitter:

a. Exocytosis

b. Endocytosis

c. Vesicles

d. Vacuoles

c. Vesicles

Release of neurotransmitter:

I. Release from the nerve terminals is through a calcium-dependent exocytosis calcium entry

II. Release in the post-ganglionic endings

III. Release in the SNS except at thermoregulatory sweat glands

IV. In the brain, majority of neurotransmitter released is Epinephrine

V. In the peripheral organ, majority is Norepinephrine which is released from adrenal medullary chromaffin cells.

a. I, II, III

b. II, III, IV

c. I, II, V

d. III, IV

e. I, II, III, IV

a. I, II, III

Release of neurotransmitter:

I) Release from the nerve terminals is through a calcium-dependent exocytosis calcium entry.

II) Release in the post-ganglionic endings

III) Release in the SNS except at thermoregulatory sweat glands.

IV) In the brain, majority of neurotransmitter released is NOREPINEPHRINE.

V) In the peripheral organ, majority is EPINEPHRINE which is released from adrenal medullary chromaffin cells.

Neurotransmitter is release in the SNS except at thermoregulatory sweat glands.

a. True

b. False

a. True

Majority of neurotransmitter in the brain.

a. Epinephrine

b. Norepinephrine

c. Dopamine

d. a and b

e. b and c

f. All

b. Norepinephrine

Majority of neurotransmitter in the peripheral organs.

a. Epinephrine

b. Norepinephrine

c. Dopamine

d. a and b

e. b and c

f. All

a. Epinephrine

Agent that can block storage of neurotransmitter:

a. Reserpine

b. Tyramine

c. Ephedrine

d. Amphetamine

e. All

a. Reserpine

Agents that can alter exocytosis of NE except:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. Tyramine

e. Reserpine

f. None

e. Reserpine

Agents that enhance exocytosis of NE except:

a. Tyramine

b. Ephedrine

c. Ampethamine

d. Methamphetamine

e. Angiotensin II

f. None

f. None

Agents that inhibits release of NE:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. All

e. None

d. All

Agents that decrease sympathetic effect:

a. Guanethedine

b. Guanadrel

c. Bretylium

d. All

e. None

d. All

Agents that increase sympathetic effect except:

a. Tyramine

b. Ephedrine

c. Ampethamine

d. Angiotensin II

e. Methamphetamine

f. None

f. None

Termination of neurotransmitter may be through:

a. Reuptake

b. Diffusion

c. Metabolism

d. a and b

e. b and c

f. All

f. All

Reuptake inhibitors:

a. Increase NE in synapse

b. Increase NE binding to receptor

c. Increase sympathetic effect

d. a and b

e. b and c

f. All

f. All

Reuptake inhibitors:

a. Cocaine

b. Atomoxetine

c. Sibutramine

d. a and b

e. b and c

f. All

f. All

Enzyme that metabolize neutrotransmitters:

a. COMT

b. MAO

c. Both

d. None

c. Both

COMT inhibitors:

a. Entacapone

b. Tolcapone

c. Selegine

d. a and b

e. b and c

f. All

d. a and b

MAO inhibitors except:

a. Moclobemide

b. Phenalzine

c. Isocarboxazid

d. Tranylcypromine

e. Selegiline

f. None

f. None

MAO A selective inhibitor:

a. Moclobemide

b. Phenalzine

c. Isocarboxazid

d. Tranylcypromine

e. Selegiline

f. None

a. Moclobemide

MAO B selective inhibitor:

a. Moclobemide

b. Phenalzine

c. Isocarboxazid

d. Tranylcypromine

e. Selegiline

f. None

e. Selegiline

Non selective MAO inhibitor:

a. Phenalzine

b. Isocarboxazid

c. Tranylcypromine

d. a and b

e. b and c

f. All

f. All

True about alpha 1 sympathetic receptor except:

a. Gq

b. AC pathway

c. Increases DAG, IP3

d. Increases calcium

e. None

b. AC pathway - It is PLC pathway

Effects of alpha 1 sympathetic receptor except:

I. Mydriasis

II. Hypertension

III. Urinary retention

IV. Ileus

v. Piloerection and ejaculation

VI. Glycogenolysis and gluconeogenesis

a. I

b. II, III

c. IV

d. III

e. None

e. None

Alpha 2 receptor except:

a. Gi

b. AC pathway

c. Increase cAMP

d. None

c. Increase cAMP - it DECREASE camp

Alpha 2 receptor effects:

a. Inhibits the presynaptic release of NE (autoregulation)

b. Aggregation of platelets

c. Inhibits insulin release causing hyperglycemia

d. a and b

e. b and c

f. All

f. All

B1 sympathetic receptor:

a. Gs

b. AC pathway

c. Increase cAMP

d. a and b

e. b and c

f. All

f. All

Location of beta 1 receptor.

a. Heart

b. Juxtaglomerular cells

c. Both

d. None

c. Both

Effects of beta 1 receptor except:

a. Increase inotropy (force of contraction) of heart

b. Increase chronotrophy (rate of contraction) of heart

c. Increase dromotrophy (conduction velocity) of heart

d. Increase renin secretion increasing synthesis of angiotensin II in juxtaglomerular cells

e. None

e. None

B2 sympathetic receptor:

a. Gs

b. AC pathway

c. Increase cAMP

d. a and b

e. b and c

f. All

f. All

Beta 2 receptor causes relaxation to:

a. Smooth muscles

b. Skeletal muscles

c. Adipose tissue

d. All

e. None

a. Smooth muscles

Effects of b2 receptor except:

I. Bronchodilation

II. GI relaxation and uterus relaxation (Tocolysis)

III. Blood vessel dilation

IV. Skeletal muscle relaxation

V. Hypokalemia: uptake of K in the skeletal muscles

VI. Glycogenolysis or gluconeogenesis

a. I

b. I, II

c. IV

d. IV, V

e. None

c. IV

Effects of b2 receptor except:

I) Bronchodilation

II) GI relaxation and Uterus relaxation (Tocolysis)

III) Blood vessel dilation

IV) Skeletal muscle CONTRACTION

V. Hypokalemia: uptake of K in the skeletal muscles

VI. Glycogenolysis or gluconeogenesis

B3 sympathetic receptor:

a. Gs

b. Located in adipose tissue

c. Can cause lipolysis leading to weight loss

d. a and b

e. b and c

f. All

f. All

Sympathomimetics

a. Agonist

b. Mimic the effects of endogenous catecholamines specifically NE, EPI

c. Usually derived from the parent compound B-phenylethylamine.

d. a and b

e. b and c

f. All

f. All

Parent compound of sympathomimetic drugs

a. a-phenylethylamine

b. B-phenylethylamine

c. a-phenylmethylamine

d. B-phenylmethylamine

b. B-phenylethylamine

Classifications of sympathomimetics.

a. Direct-acting

b. Indirect-acting

c. Mixed-acting

d. a and b

e. b and c

f. All

f. All

Classifications of sympathomimetics:

1) Directly activate postjunctional and prejunctional adrenoceptors

2) The drug will directly bind into the receptor = ↑ Sympathetic effect

a. Direct-acting

b. Indirect-acting

c. Mixed-acting

a. Direct-acting

Classifications of sympathomimetics:

1) Promote sympathetic effects by either enhancing release or preventing reuptake of NE

2) The natural Norephedrine will bind to the receptor

a. Direct-acting

b. Indirect-acting

c. Mixed-acting

b. Indirect-acting

Classifications of sympathomimetics:

Possess both direct and indirect actions

a. Direct-acting

b. Indirect-acting

c. Mixed-acting

c. Mixed-acting

More common indirect mechanism of indirect enhancement of sympathetic effect for mixed acting sympathomimetic drugs.

a. enhancing release of NE

b. preventing reuptake of NE

c. Equally used

d. None

a. enhancing release of NE

Non-selective direct acting agents:

a. Activate more than 1 general type of sympathetic receptors.

b. Both alpha and beta, or both alpha, beta, dopa.

c. Never activate one type or receptor alone.

d. a and b

e. b and c

f. All

f. All

Non-selective direct acting agents:

a. Epinephrine

b. Norepinephrine

c. Dopamine

d. a and b

e. b and c

f. All

f. All

Natural catecholamines except:

a. Undergo extensive first pass effect thus poorly absorbed in the GIT and in the CNS

b. Poor oral bioavailability thus NOT taken by mouth

c. Mostly administered IV, Inhalation, Subcutaneous with caution to avoid cardiac arrhythmias or local tissue necrosis

d. Metabolized extensively by COMT and MAO

e. It is nonpolar thus it can pass BBB and have CNS effect.

f. None

e. It is nonpolar thus it can pass BBB and have CNS effect

It is POLAR thus it CANNOT pass BBB and DON’T HAVE CNS effect.

Epinephrine:

I. Adrenaline

II. Activates B1-, B2-, and a-receptors

III. Causes vasoconstriction (high doses) and coronary blood flow

IV. Increases the drainage of aqueous humor thus used as antiglaucoma

V. Relaxes bronchial smooth muscles

a. I, II, III

b. II, III, IV

c. I, II, V

d. III, IV

e. I, II, III, IV, V

f. II, III, IV, V

e. I, II, III, IV, V

Epinephrine:

I) Adrenaline

II) Activates B1-, B2-, and a-receptors

III) Causes vasoconstriction (high doses) and coronary blood flow

IV) Increases the drainage of aqueous humor thus used as antiglaucoma

V) Relaxes bronchial smooth muscles

Depivefrine is anti-glaucoma agent which is the pivalic acid ester of what neurotransmitter?

a. Norepinephrine

b. Epinephrine

c. Dopamine

d. Reserpine

e. None

b. Epinephrine

Norepinephrine except:

a. Activates B1-receptors and alpha receptors with little activity at B2-receptors

b. More used as bronchodilator

c. Rarely used therapeutically

d. Noradrenaline

e. a and c

f. All

b. More used as bronchodilator

Norepinephrine:

a) Activates B1-receptors and alpha receptors with little activity at B2-receptors.

b) NOT used as bronchodilator

c) Rarely used therapeutically

Dopamine:

a. Activates peripheral B1-adrenoceptors, pre-junctional and post-junctional dopamine D1-receptors in the renal, coronary, and splanchnic vessels.

b. Has positive inotropic effect at low doses

c. Causes vasoconstriction at high doses

d. a and b

e. b and c

f. All

f. All

Dopamine activates pre-junctional and post-junctional dopamine D1-receptors in which of the following vessels?

a. renal

b. coronary

c. splanchnic

d. a and b

e. b and c

f. All

f. All

Dopamine activation of D1 receptor in the renal vessels:

a. Vasodilation

b. Increases GFR

c. Promote diuresis

d. a and b

e. a and c

f. All

f. All

Dopamine has positive inotropic effect at?

a. Low doses

b. High doses

c. All doses

a. Low doses

Dopamine has vasoconstriction effect at?

a. Low doses

b. High doses

c. All doses

b. High doses

Selective sympathomimetic drugs

a. Targets specific sympathetic receptors

b. Either alpha or beta only

c. Both

d. None

c. Both

Non-selective B Agonist

a. Dobutamine

b. Terbutaline

c. Isoproterenol

d. Isoprenaline

e. a and b

f. c and d

f. c and d

Isoprenaline is the brand of Isoproterenol

B1 selective Agonist

a. Dobutamine

b. Terbutaline

c. Isoproterenol

d. Albuterol

e. Metaproterenol

f. PirbuterolB

a. Dobutamine

Dobutamine route of administration.

a. IV infusion

b. SC

c. IM

d. Oral

a. IV infusion

B2 selective agonist

a. Relax bronchial smooth muscles

b. Selectivity is lost at high concentrations thus can have side effect of tachycardia

c. Can be short or long acting

d. a and b

e. b and c

f. All

f. All

Short acting B2 selective agonist except

a. Salmeterol

b. Terbutaline

c. Albuterol

d. Metaproterenol

e. Pirbuterol

f. None

a. Salmeterol - this is LONG acting

Long acting B2 selective agonist except:

a. Salmeterol

b. Formoterol

c. Indacaterol

d. Bambuterol

e. Albuterol

f. None

e. Albuterol - this is SHORT acting

Uses of B2 selective agonist

a. Bronchodilator

b. Treatment of bronchial asthma and COPD

c. Tocolytics

d. For preterm labor

e. All

f. None

e. All

B2 selective agonist used at tocolytics

a. Ritoridine

b. Isoxuprine

c. Terbutaline

d. a and b

e. b and c

f. All

f. All

B2 selective agonist with off label use as tocolytic

a. Ritoridine

b. Isoxuprine

c. Terbutaline

d. a and b

e. b and c

f. All

c. Terbutaline

The only SC B2 agonist.

a. Terbutaline

b. Bambuterol

c. Albuterol

d. Salmeterol

a. Terbutaline

Oral B agonist.

a. Terbutaline

b. Bambuterol

c. Albuterol

d. Salmeterol

b. Bambuterol

Salbutamol

a. Terbutaline

b. Bambuterol

c. Albuterol

d. Salmeterol

c. Albuterol

Constrictor drugs

a. Selective A1 agonist

b. Selective A2 agonist

a. Selective A1 agonist

Lower BP due to activation of inhibitory receptors

a. Selective A1 agonist

b. Selective A2 agonist

b. Selective A2 agonist

Selective A1 agonist except:

a. Phenylephrine

b. Methoxamine

c. Metaraminol

d. Xylometazoline

e. Oxymetazoline

f. None

f. None

Not metabolized by COMT

Less potent

Longer of DOA

Can be oral

I. Phenylephrine

II. Methoxamine

III. Metaraminol

IV. Xylometazoline

V. Oxymetazoline

a. I, II

b. I, II, III

c. III, IV

d. III, IV, V

e. IV, V

b. I, II, III - Vasoconstrictor selective A1 agonist

Nasal decongestant

May cause Clonidine-like effects at high doses.

I. Phenylephrine

II. Methoxamine

III. Metaraminol

IV. Xylometazoline

V. Oxymetazoline

a. I, II

b. I, II, III

c. III, IV

d. III, IV, V

e. IV, V

e. IV, V

Xylometazoline and Oxymetazoline

a. Nasal decongestant

b. Used for 3 days only

c. Beyond 3 days, it will cause rebound congestion or rhinitis medica mentosa

d. a and b

e. b and c

f. All

f. All

Selective A2 agonist

a. Lower BP due to activation of inhibitory receptors

b. Directly inactivate pre-junctional alpha2 receptors in the vasomotor center of the medulla

c. Reduce sympathetic tone thus reducing blood pressure

d. a and b

e. b and c

f. All

f. All

Selective A2 agonist except:

a. Clonidine

b. Methyldopa

c. Guanabenz

d. Guanfacine

e. None

e. None

Selective A2 agonist that is not used anymore

a. Clonidine

b. Methyldopa

c. Guanabenz

d. Guanfacine

e. a and b

f. c and d

f. c and d

Methyldopa except:

a. Aldomet

b. Prodrug → a-methylnorepinephrine

c. False neurotransmitter

d. Safe for the treatment of hypertension for pregnant women

e. None

e. None

Toxicity or side effects of methyldopa

a. Sedation

b. False positive Coomb's test

c. False postive for hemolytic anemia

d. a and b

e. b and c

f. All

f. All

Antihypertensive drugs safe for pregnancy except:

a. Methyldopa

b. Hydralazine

c. Labetalol

d. Nicardipine

e. Nifedipine

f. None

d. Nicardipine

Clonidine except:

a. Catapres

b. Has initial effect of vasoconstriction increasing BP

c. Has lasting effect of vasodilation reducing BP

d. Has a side effect of rebound hypertension

e. b and c

f. None

f. None

A2 agonist that can be used for glaucoma

a. Methyldopa

b. Apraclonidine

c. Brimonidine

d. a and b

e. b and c

f. All

e. b and c

Indirect acting sympathomimetic drugs has the mechanisms

a. Enhancing exocytosis

b. Reuptake inhibitors

c. Both

d. None

c. Both

Enhance exocytosis

a. Tyramine

b. Ephedrine

c. Amphetamine

d. a and b

e. b and c

f. AllT

f. All

True statements except:

a. Ephedrine and mephentermine are less potent than EPI

b. Ephedrine and mephentermine are resistant to metabolism by MAO and COMT thus have long DOA

c. Ephedrine is found in Ma Huang

d. Pseudoephedrine is isomer of ephedrine

e. None

f. All

e. None

Describe mixed-acting sympathomimetic drugs except:

a. Possess both direct and indirect actions

b. Has CNS effect because they are nonpolar and can enter the BBB

c. Resistant to COMT & MAO as they are non-catecholamines thus has long duration of action

d. Can be habit forming or has chances of addiction

e. Enter CNS readily and have marked stimulant activity

f. None

f. None

Mixed-acting sympathomimetic drugs except:

Dextroamphetamine

Amphetamine

Methamphetamine

Phendimetrazine

Methylphenidate

Modafinil

Hydroxyamphetamine

a. Methamphetamine

b. Hydroxyamphetamine

c. Amphetamine

d. Phendimetrazine

e. None

e. None

Mixed-acting sympathomimetic drug that cannot enter the CNS readily.

a. Methamphetamine

b. Hydroxyamphetamine

c. Amphetamine

d. Phendimetrazine

e. Modafinil

b. Hydroxyamphetamine

Sympathomimetic drugs for cardiovascular conditions.

I. Phenylephrine

II. Methoxamine

III. Norepinephrine

IV. Ephedrine

V. Midodrine

a. I, II

b. I, II, III

c. IV

d. IV, V

e. I, II, III, IV, V

e. I, II, III, IV, V

Sympathomimetic drugs for short-term hypotensive emergencies.

I. Phenylephrine

II. Methoxamine

III. Norepinephrine

IV. Ephedrine

V. Midodrine

a. I, II

b. I, II, III

c. IV

d. IV, V

e. I, II, III, IV, V

b. I, II, III

Sympathomimetic drugs for chronic orthostatic hypotension.

I. Phenylephrine

II. Methoxamine

III. Norepinephrine

IV. Ephedrine

V. Midodrine

a. I, II

b. I, II, III

c. IV

d. IV, V

e. I, II, III, IV, V

d. IV, V

Low to moderate doses is for cardiogenic or septic shock, CHF.

a. Dobutamine or Dopamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

a. Dobutamine or Dopamine

First line for cardiogenic shock caused by heart failure.

a. Dobutamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

f. Dopamine

a. Dobutamine

For septic shock or extreme hypotension caused by infection.

a. Dobutamine or Dopamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

b. Norepinephrine

For anaphylactic shock or extreme hypotension caused by allergy.

a. Dobutamine or Dopamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

c. Epinephrine

For hypertension in pregnancy.

a. Dobutamine or Dopamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

d. Methyldopa

D1 agonist which is for severe HTN.

a. Dobutamine or Dopamine

b. Norepinephrine

c. Epinephrine

d. Methyldopa

e. Fenoldopam

e. Fenoldopam