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from : learn pharmacology in ten days book > Adrenergic drugs > Flashcards

Adrenergic drugs Flashcards

1
Q

Chemical classification of adrenergic drugs ?

A

Catecholamines (natural and synthetic) &non-catecholamines.

  • Catecholamines :
  • Natural catecholamines : Adrenaline
  • Synthetic catecholamines : Dobutamine,
  • Non-catecholamines : Amphetamine,
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2
Q

More detailed classification of adrenergic drugs ?

A

Catecholamines (natural and synthetic) &non-catecholamines.

  • Catecholamines :
  • Natural catecholamines : Adrenaline, Noradrenaline and Dopamine.
  • Synthetic catecholamines : Dobutamine, Isoetherine, Isoprenaline, Hexaprenaline, Rimiterol.
  • Non-catecholamines : Amphetamine, Dexamphetamine, Terbutaline, Ephedrine, Pseudoephedrine, Metaraminol.
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3
Q

Classification of adrenergic drugs according to their mechanism of action ?

A
  • Directly acting sympathomimetics
  • Directly and indirectly acting sympathomimetics
  • Indirectly acting symathomimetics :
  • Release of Noradrenaline
  • Reuptake of inhibitors
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4
Q

Classification of adrenergic drugs based on receptors selectivity ?

A

based on receptors selectivity :

  • alpha 1 agonists
  • alpha 2 agonists
  • alpha 1 &2 agonists
  • beta 1 agonists
  • beta 2 agonists
  • beta 1 &2 agonists
  • adrenergic &dopaminergic agonists
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5
Q

What are the natural catocholamines ?

A

Adrenaline, Noradrenaline and Dopamine.

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6
Q

Synthetic catecholamines ?

A

Dobutamine, Isoetherine, Isoprenaline, Hexaprenaline, Rimiterol.

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7
Q

Non-catecholamines ?

A

Amphetamine, Dexamphetamine, Terbutaline, Ephedrine, Pseudoephedrine, Metaraminol.

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8
Q

Directly acting sympathomimetics ?

A

Terbutaline, Salbutamol, Adrenaline, Noradrenaline, Isoprenaline.

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9
Q

Directly and indirectly acting sympathomimetics ?

A

Ephedrine, Metaraminol.

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10
Q

Indirectly acting symathomimetics; release of Noradrenaline ?

A

Amphetamine, Methylamphetamine, Tyramine.

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11
Q

Indirectly acting symathomimetics; reuptake of inhibitors ?

A

Cocaine, Tricyclic antidepressants.

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12
Q

alpha-1 agonists ?

A

Methoxamine, Xylometazoline, Phenylephrine.

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13
Q

alpha 2 agonists ?

A

a-methyldopa, Clonidine

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14
Q

alpha 1 &2 agonists ?

A

Oxymetazoline

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15
Q

beta 1 agonists ?

A

Prenalterol, Dobutamine.

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16
Q

beta 2 agonists ?

A

Salbutamol, Terbutaline, Fenterol, Prenalterol.

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17
Q

beta 1 &2 agonists ?

A

Isoprenaline, Orciprenaline

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18
Q

adrenergic &dopaminergic agonists ?

A

Dopamine

19
Q

Sympathomimetics effects on the eye ?

A

alpha-1 receptors :
Mydriasis
Distant accommodation

20
Q

Sympathomimetics effects on the bronchi ?

A

beta-2 receptors :

Bronchodilation.

21
Q

Sympathomimetics effects on the heart ?

A

beta-1 receptors :

Increase of heart rate &contractility.

22
Q

Sympathomimetics effects on blood vessels ?

A

alpha-1 :
Contraction of renal and dermal vessels (primarily)
beta-2 :
Peripheral vasodilation

23
Q

Sympathomimetic effects on the GIT ?

A

alpha-1 :
Sphincter contraction (Includes the upper and lower esophageal, pyloric, and anal sphincters)
beta-2 :
decrease of peristalsis

24
Q

Sympathomimetic effects on bladder ?

A

alpha-1 :
Sphincter contraction
beta-2 :
Detrusor relaxation (bladder is able to store urine)

25
Q

on skeletal muscles ?

A

beta-2 :
↑ Contraction
↑ Glycogenolysis

26
Q

On adipose tissues ?

A

beta-2 (yes)

↑ Lipolysis

27
Q

On kidneys ?

A

beta-1 :

↑ Release of renin

28
Q

Now direct sympathomimetics, specifically alpha-1 agonists side effects?

A
  • Hypertension (due to peripheral vasoconstriction) and reflex bradycardia
  • Piloerection
  • Urinary retention
  • Ischemia and necrosis, especially of the fingers or toes; in some cases, organ involvement (e.g., intestinal or kidney injury)
29
Q

Directly sympathomimetics, alpha-2 agonists side effects ?

A

Side effects of alpha-2 agonists are mainly due to their sympatholytic effects :

  • CNS depression (e.g., sedation)
  • Respiratory depression
  • Bradycardia and -hypotension
  • Miosis
  • Rebound hypertension
  • Dry mouth
  • alpha-methyldopa side effects :
  • Autoimmune hemolytic anemia
  • SLE-like syndrome (Systemic lupus erythematosus)
30
Q

beta-1 agonists side effects ?

A

Tachycardia and arrhythmias

Can precipitate angina or myocardial infarction in patients with coronary artery disease

31
Q

Beta-2 agonists side effects ?

A

Tremor (most common side effect), agitation, insomnia, diaphoresis
Hypotension (due to peripheral vasodilation) and reflex tachycardia
Metabolic disturbances: hyperglycemia, hypokalemia

32
Q

Indirect sympathomimetics, ephedrine side effect ?

A
  • Hypertension
  • Reflex bradycardia (due to hypertension) or -tachycardia
  • Dizziness
  • Nausea, vomiting
33
Q

Brief description of sympathomimetics and their effects ?

A

Sympathomimetics are substances that mimic or modify the actions of endogenous catecholamines of the sympathetic nervous system. Direct agonists directly activate adrenoceptors, while indirect agonists enhance the actions of endogenous catecholamines. α, β, and dopamine (D) receptors are stimulated in various target tissues such as the eyes, heart, and vascular smooth muscle. The clinical indications for sympathomimetics are broad and include asthma, heart failure, shock, and anaphylaxis. Side effects include hypertension, sinus tachycardia, and skeletal muscle tremor.

34
Q

Salbutamol indication ?

A
  • Asthma

- COPD

35
Q

Dobutamine indication ?

A

Heart failure : At high doses, dobutamine acts preferentially as a beta agonist. Therefore, in patients with heart failure, high-dose dobutamine is useful because it increases cardiac output (due to an increase in heart rate as well as contractility by β1 agonism) and decreases cardiac afterload (due to peripheral vasodilation by β2 agonism). IV epinephrine is used if the patient is hemodynamically unstable and requires cardiopulmonary resuscitation.

36
Q

Dopamine indications ?

A

Heart failure
Shock
Unstable bradycardia (Chronotropic effects at lower doses (β effect); vasoconstriction at high doses (α effect))

37
Q

Epinephrine indications ?

A
  • Asthma
  • Open-angle glaucoma
  • Anaphylaxis
38
Q

Phenylephrine indications ?

A
  • Hypotension
  • Rhinitis
  • Allergic conjunctivitis
  • Open-angle glaucoma
39
Q

Present a brief passage about alpha-2 receptors ?

A

Alpha 2 receptors in the brain stem and in the periphery inhibit sympathetic activity and thus lower blood pressure. Alpha 2 receptor agonists such as clonidine or guanabenz reduce central and peripheral sympathetic overflow and via peripheral presynaptic receptors may reduce peripheral neurotransmitter release.

40
Q

Where are smooth muscle alpha-1 receptors present ?

A

In smooth muscle cells of blood vessels the principal effect of activation of these receptors is vasoconstriction. Blood vessels with alpha1-adrenergic receptors are present in the skin, the sphincters of gastrointestinal system, kidney (renal artery) and brain. During the fight-or-flight response vasoconstriction results in decreased blood flow to these organs. This accounts for the pale appearance of the skin of an individual when frightened.

41
Q

Phenylpropanolamine ?

A

Sympathomimetic (alpha-1) used as decongestant &appetite suppressant.

Activation of α1-adrenergic receptors produces anorexia and partially mediates the efficacy of appetite suppressants like phenylpropanolamine and amphetamine

42
Q

An effect of alpha-1 agonists relatively similar to b-2 agonists ?

A

Alpha–1 agonists induce contraction of the urinary bladder although this effect is minor compared to the relaxing effect of β2-adrenergic receptors. In other words, the overall effect of sympathetic stimuli on the bladder is relaxation, in order to inhibit micturition upon anticipation of a stressful event.

43
Q

Alpha-1 adrenergic drugs cause contraction in ?

A
  • Bladder
  • Ureter
  • Uterus (when pregnant)
  • Urethral sphincter
  • Bronchioles (although minor to the relaxing effect of beta-2 receptor on bronchioles)
  • Iris dilator muscle
  • Seminal tract, resulting in ejaculation.

from : learn pharmacology in ten days book (8 decks)

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