CNS: Anthraquinones and MAO Inhibitors

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18 Questions

What is the effect of Hypericin on neurotransmitters?

Increase epinephrine, serotonin and dopamine

What is the advantage of hypnotics and sedatives from plant origin?

Mild in their action, low risk of overdose and no risk of tolerance, habituation or addiction

What is the effect of Valerian on GABA?

Stimulate synthesis and release of GABA

What is the effect of Caffeine on Adenosine receptors?

Antagonist

What is the effect of Passion flower on neurotransmitters?

Increase the release of GABA

What is the effect of Kavalactones on GABA?

Increase the binding sites of GABA

What is the mechanism of action of Narcotic Analgesics?

Mimic the action of endogenous opioids at receptors, inhibiting the release of neurotransmitters

What is the treatment for Depression?

St John wort and Passion flower

What is the effect of Feverfew on Arachidonic acid synthesis?

Decrease Arachidonic acid synthesis

What is the effect of Hyperforin on GABA?

Increase GABA release and inhibit reuptake and catabolism

What is the main characteristic of Alzheimer's disease?

Irreversible and progressive brain disease

What is the active compound found in Calabar beans used to treat Alzheimer's disease?

Physostigmine

What is the effect of Ginkgolides A and B on platelet-activating factor?

Antagonist

What is the side effect of Ginkgo biloba that requires dose adjustment in diabetic patients?

Hypoglycemia

What is the herb used to treat numbness in feet in the given case study?

Capsicum

What is the effect of Ginkgo biloba on tau protein phosphorylation?

Decreases

What is the common symptom of depression in the given case study?

Lack of self-esteem

What is the herb used to treat insomnia in the given case study?

Valerian

Study Notes

CNS Depressants

  • Anthraquinones (Hypericin) from St John's Wort inhibit MAO, increasing epinephrine, serotonin, and dopamine
  • Hyperforin decreases GABA binding to receptors
  • Side effects: activating CYP 450, reducing concentrations of anticonvulsants, theophylline, contraceptives, and warfarin
  • Contraindications: pregnancy, lactation
  • Dosage form: Tablets (300 mg)

Valerian

  • Sesquiterpene volatile oils (0.8% Valerianic acid) stimulate GABA synthesis and release
  • Inhibit GABA reuptake and catabolism, increasing extracellular GABA concentrations
  • Side effects: severe depression, cardiac function disturbance (high dose)
  • Contraindications: pregnancy, children (oxytocic due to Iridoids)
  • Dosage form: Infusion (2-3 gm) at bedtime

Passion Flower

  • Gama-Pyrone derivatives (Maltol & Ethyl maltol) and Flavonoids C-glycosides (vitexin) have affinity for GABA receptors
  • Increase GABA release and inhibit reuptake and catabolism (CNS depressant)
  • Monoamine oxidase inhibition effect (can be used as an antidepressant, CNS stimulant)
  • Side effects: uterine stimulant, not used in pregnancy
  • Certain aminoglycosides (Clindamycin) potentiate the relaxing action of Passion flower

Kava

  • Kavalactones (Kavapyrones): Kavain, Methysticin, and Yangonin increase GABA binding sites
  • Inhibit noradrenaline uptake and catabolism, leading to mood elevation and depression treatment
  • Side effects: dermopathy (reversible yellow discoloration), liver damage
  • Interactions: diuretics, alcohol, and other depressants may potentiate the action of Kava
  • Dosage form: Decoction (1.5-3 gm) at bedtime

Hops

  • Alpha acid (Humulone) and Beta acid (Lupulone) increase GABA release and receptors
  • Side effects: menstrual cycle disturbance, not used in pregnancy
  • Dosage form: Decoction (1-2 gm) at bedtime

Narcotic Analgesics

  • Opiate alkaloids derived from opium (dried exudates of poppy capsule, Papaver somniferum)
  • Examples: Morphine, Levorphanol, Methadone, Fentanyl
  • Mechanism: mimics the action of endogenous opioids at receptors, inhibiting release of neurotransmitters
  • Therapeutic indications: relieve pain associated with myocardial infarction, cancer, and post-operation
  • Side effects: sedation, miosis, depression, respiratory depression, constipation, biliary spasm, hypotension, euphoria, and dependence

Feverfew

  • Sesquiterpene Lactone (Parthenolide) inhibits Arachidonic acid synthesis, prostaglandin and leukotriene synthesis
  • Decreases smooth muscle spasm, inhibits platelet aggregation, and histamine release (anti-allergic) and serotonin secretion
  • Side effects: mouth ulcers, tongue swelling, bleeding disorders with warfarin
  • Contraindications: patients hypersensitive to drugs of family Asteraceae (Chamomile)
  • Dosage form: 50-250 mg daily

Ginkgo Biloba

  • 6% Terpene (Ginkgolides) and 24% flavonoids
  • Ginkgolides A and B are platelet-activating factor antagonists and neuro-protective
  • Inhibit monoamine oxidase (increase dopamine and acetylcholine), protect against amyloid peptide synthesis
  • Relieve cerebral ischemia and prevent memory deterioration (dementia)
  • Side effects: ototoxicity with aminoglycosides, hypoglycemia, bleeding, hypertension, loss of appetite
  • Dosage forms: Tablets, Capsules, Syrup

This quiz covers the effects of anthraquinones, specifically Hypericin, on the central nervous system, including its role as a MAO inhibitor and its impact on neurotransmitters such as epinephrine, serotonin, and dopamine.

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