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INT 208: Pharmacology > Autonomic NS 5: Ephedrine & Amphetamine > Flashcards

Autonomic NS 5: Ephedrine & Amphetamine Flashcards

1
Q

Chemistry of Ephedrine

A

Natural alkaloid from ephedra plant

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2
Q

oral adminstration of Ephedrine

A

effective & stable

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3
Q

Ephedrine can be injected ____

A

subcutaneous & intramuscular

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4
Q

Local eye drop of ephedrine

A

diffusion can occur

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5
Q

Describe distribution of ephedrine

A

can pass blood brain barrier & have an effect on CNS

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6
Q

Describe metabolism of ephedrine

A

Generally: slow metabolism with long duration
* Metabolized only by the liver
* not destroyed by MAO (as it is not a Catecholamine)
* May even inhibit MAO (so shouldn’t be given with MAO inhibitors)

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7
Q

Describe excretion of Ephedrine

A
  • in urine
  • Mainly unchanged
  • Acidification of urine increases its renal excretion
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8
Q

renal Excretion of Ephedrine can be increased by

A

Acidification of Urine

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9
Q

difference between Ephedrine & Adrenaline (epinephrine) in duration

A

Ephedrine has longer duration, due to it not being broken down by MAO

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10
Q

difference between Ephedrine & Adrenaline (epinephrine) in Distribution

A
  • Ephedrine can be absorbed orally (through GIT), adrenaline can’t
  • Ephedrine can pass BBB thus has an effect on CNS, adrenaline doesn’t
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11
Q

difference between Ephedrine & Adrenaline (epinephrine) in local application on the eyes

A
  • Ephedrine causes Mydrasis
  • Adrenaline has no effect when applied locally on the eye due to no diffusion
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12
Q

Mixed acting sympathomemtic

A

Ephedrine

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13
Q

effect of repetitive adminstration of ephedrine

A
  • Tolerence
  • Tachyphylaxis (decreased response) ( effect is reduced due to depletion of NA vesicles)
  • (at short intervals) dimenishes/ removes the hypertensive response
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14
Q

Explain why, despite having similar pharmacodynamics, ephedrine is contraindicated with enlarged prostate, but Adrenaline isn’t

A

Adrenaline is a Catecholamine, which means it can be broken down by MAO, therefore its effect is rapid with shorter duration, thus wont affect urine retention

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15
Q

Action of Ephedrine

A

stimulates Alpha & Beta with longer duration than adrenaline, and weaker effect on Beta

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16
Q

Mechanism of Ephedrine

A

Dual Action:
* direct: acts on Alpha & Beta
* Indirect: facilitates release of NA from vesicles

Mainly indirect

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17
Q

effect of Ephedrine on heart

A

Increase all cardiac properties

Like adrenaline

18
Q

effect of Ephedrine on Blood vessels

A
  • general Vasoconstriction of skin & mucosal membrane (alpha 1)
  • Vasodilatation of Cornary & skeletal vessels (Beta1)
19
Q

effect of Ephedrine on blood pressure

A

(noradrenaline mota5afy= weak Beta, strong alpha)
* Elevate both systolic and diastolic blood pressure
* when given with alpha blocker, there is no reversal/ no beta effect
* Alpha blockers completely abolish pressor effect when given with Epherine

20
Q

effect of Ephedrine on smooth muscles

A

Same as Epinephrine/ Adrenaline
* eye–> mydrasis
* Bronchi—> bronchdilatation
* Urinary tract—-> relaxation of wall
* Sex organs —–> male=ejaculation

21
Q

effect of Ephedrine on Skeletal muscle

A
  • Facilitate Neuromuscular transmission
  • Causes Vasodilatation of skeletal vessels Used to treat Myasthenia gravis (long duration)
22
Q

Explain why ephedrine is used to treat myathenia gravis but adrenaline isn’t

A

despite both causing Vasodilatation of skeletal blood vessels, Adrenaline is broken down by MAO, Ephedrine isn’t, therfore it has a duration long enough to treat gravis

23
Q

Describe effect of ephedrine on CNS

A
  • Analeptic= stimulates respiratory & vasomotor centers in CNS (used in treating morphine overdose)
  • stimulates Cerebral cortex & reticular formation (causes anxiety & insomnia)
24
Q

Local use of Ephedrine

A
  • Epistaxis (Hemostatic effect)
  • Nasal decongestant (pseudoephedrine is better to avoid irritation)
  • Mydrasis (local on eye)
25
Q

CVS use of Ephedrine

A
  • Heart block
  • Before spinal anesthesia (elevate bp)
26
Q

Respiration use for Ephedrine

A

Bronchial asthma

27
Q

ephedrine is used in treatement of Myasthenia gravis together with____

A

Neostigmatine

28
Q

CNS use of Ephedrine

A
  • Nocturnal Enuresis
  • Narcolepsy
  • Morphine toxicity affecting respiratory & vasomotor centers (analeptic)
29
Q

Side effect of Ephedrine

A

like adrenaline +:
* Insomnia
* Anxiety
* Retention of urine (in enlarged prostate patients)
* Tolerence & tachyphylaxis (without addiction)

30
Q

Tyramine is present in

A
  • Yoghurt
  • Cheese
31
Q

Tyramine metabolism

A

broken down by MAO

32
Q

tyramine mechanism

A

release NA from vesicles (indirect)

33
Q

Clinical importance regarding Tyramine

A

in pateints taking MAO inhibitors, it’s not broken down, thus causes Hypertensive crisis

AKA “Cheese reaction”

34
Q

Hypertension caused by unrestricted activity of Tyramine (inhibiting MAO) is solved by

A

Alpha Blocker

35
Q

effect of reserpine

A

depletion of stored NA & Serotonin

tyramine has no more action on serotonin and depression treatement

36
Q

effect of Amphetamine on psych depending on dose

A

small dose:
* Alertness
* Euphoria
* Delay mental fatigue
* when effect deminished, it’s followed by fatigue & depression

Moderate dose:
* Anxiety
* tremors

Large dose:
* paranoid type Schizophrenia
* Hyperpyrexia
* Convulsions

Addictive

37
Q

effect of Amphetamine on CNS

A
  1. Psych: depending on dose
  2. Anorexigenic: inhibits feeding center & decreases acuity of smell & taste
  3. Analpetic: stimulates respiratory & Vasomotor centers
  4. Spinal: facilitates reflexes (mon & polysynaptic)
38
Q

Amphetamine substiute for Narcolepsy

A

Modafinil

39
Q

Medication of ADHD

A

Methylphenidate

40
Q

Side effect of Amphetamine

A
  • Insomnia
  • Anxiety
  • Anorexia
  • Addiction
  • Tachyphylaxis
  • Tolerance

INT 208: Pharmacology (30 decks)

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