Pharmacy: Central Nervous System

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Questions and Answers

What percentage of flavonoid glycosides are present in Ginkgo biloba leaves?

40-45%

30-35%

22-27% (correct)

10-15%

What is the 5th leading cause of death in elderly patients 65 years of age and older?

Alzheimer's disease (correct)

Stroke

Heart disease

Cancer

What is the role of ginkgo biloba in improving brain circulation?

Increases vasodilation

Inhibits platelet activating factor (correct)

Increases platelet activating factor

Decreases serotonin release uptake

What is the percentage of ginkgolides A, B, and C present in Ginkgo biloba leaves?

2.8-3.4% Signup and view all the answers

What is the estimated proportion of dementia cases accounted for by Alzheimer's disease?

Three-quarters Signup and view all the answers

What is the effect of ginkgo biloba on muscarinergic cholinoceptors and α-adrenoceptors?

Decreases Signup and view all the answers

What is the role of ginkgo biloba in neuroprotection?

Decreases nitric oxide formation Signup and view all the answers

What are the key pathological marks of Alzheimer's disease?

Plaques and neurofibrillary tangles Signup and view all the answers

What is the possible adverse effect of extended consumption of large doses of kava?

Scaly, yellowing skin condition Signup and view all the answers

What is the part used in valerian?

Root Signup and view all the answers

What is the mechanism of action of valerian extracts?

Allosteric modulation of GABA-A receptors Signup and view all the answers

What is the requirement for dried valerian root?

At least 0.5% volatile oil and 0.05% valerenic acid Signup and view all the answers

What is the effect of valerian on judgment and driving ability?

Mild impairment for two to three hours Signup and view all the answers

What is the possible interaction of valerian with other substances?

Potentiation of sedative effects of barbiturates Signup and view all the answers

What is the recommended dosage of valerian as a sleep aid?

Single dose ½ to 1 hour before bedtime Signup and view all the answers

What is the scientific name of passion flower?

Passiflora incarnata Signup and view all the answers

What is the recommended daily dose of Ginkgo biloba powder for dementia?

120-240 mg Signup and view all the answers

What is the scientific name of Moringa?

Moringa olifera Signup and view all the answers

What is the effect of kava on the limbic system?

It selectively acts on the limbic system, promoting anxiolysis without sedation. Signup and view all the answers

What is the interaction between kava and alprazolam?

Kava interacts with alprazolam, causing coma. Signup and view all the answers

What is the contraindication of kava in terms of mental health?

Depression Signup and view all the answers

What is the mechanism of anxiety related to?

Dysregulation of serotonergic, noradrenergic, glutamatergic and GABA-ergic transmission. Signup and view all the answers

What are the antioxidants found in Moringa leaves?

Myricetin and kaempferol Signup and view all the answers

What is the effect of kava on medications for Parkinson's disease?

Kava may counter the effects of dopamine and reduce the effectiveness of medications for Parkinson's disease. Signup and view all the answers

What is the primary mechanism of action of chrysin in passion flower?

It binds to benzodiazepine receptors and acts as an agonist for GABA activity Signup and view all the answers

What is the typical age range when melatonin levels start to decline?

Around the time of puberty Signup and view all the answers

What is the primary receptor subtype involved in melatonin's sleep-promoting action?

MT1 receptor subtype Signup and view all the answers

What is the recommended duration of melatonin treatment?

Up to 4 weeks Signup and view all the answers

Which of the following drugs can increase serum melatonin levels?

Ciprofloxacin Signup and view all the answers

What is the effect of melatonin on sleep architecture?

Marginal alteration Signup and view all the answers

What is the recommended timing for melatonin administration?

30-60 minutes before bedtime Signup and view all the answers

What is the effect of NSAIDs on endogenous melatonin production?

Suppression Signup and view all the answers

What is the primary purpose of b-blockers and pizotifen in the treatment of migraine?

To prevent recurrences of migraine Signup and view all the answers

What is the potential risk of using feverfew in pregnant women?

Increased risk of miscarriage or premature delivery Signup and view all the answers

What is the primary mechanism by which feverfew is believed to exert its antimigraine activity?

Prostaglandin inhibition Signup and view all the answers

What is the scientific name of the plant from which feverfew is extracted?

Tanacetum parthenium Signup and view all the answers

What is the primary limitation of using ergotamine in the treatment of migraine?

Severe adverse reactions Signup and view all the answers

What is the conclusion of the third meta-analysis on the efficacy of feverfew in migraine patients?

Feverfew extracts have not been proved to prevent migraine better than placebo Signup and view all the answers

What is the primary indication for using ergotamine in migraine treatment?

Acute attacks of migraine that cannot be controlled with other drugs Signup and view all the answers

What is the primary constituent of feverfew that is responsible for its antimigraine activity?

Parthenolide Signup and view all the answers

Study Notes

Central Nervous System

The plant kingdom has compounds that can stimulate or calm the CNS, with some having high-potency compounds that can be chemically isolated and used in phytotherapy.

Alzheimer Disease

Alzheimer's disease is a neurodegenerative disease characterized by cognitive and memory decline, accounting for three-quarters of all dementia cases and being the 5th leading cause of death in elderly patients.
The key pathological marks of AD are plaques and neurofibrillary tangles.
The main reasons for Alzheimer's disease are elevated levels of oxidative stress in the brain, formation of β-amyloid plaques, and depositions of neurofibrillary tangles in the hippocampus and cerebral cortex.

Ginkgo Biloba

Scientific name: Ginkgo biloba
Part used: leaves
Constituents: flavonoid glycosides (quercetin, kaempferol, and isorhamnetin) and terpene lactones (ginkgolides A,B,C and bilobalide)
Mechanisms of action:
- Improves brain circulation by inhibiting platelet activating factor and vasodilation
- Increases serotonin release and uptake
- Reduces muscarinergic cholinoceptors and α-adrenoceptors
- Acts as a free-radical scavenger and inhibits nitric oxide formation
Drug-herb interaction: may interact with warfarin, but results do not indicate a higher risk of bleeding with standardized preparation
Dose: 120-240 mg/day for dementia

Moringa

Scientific name: Moringa olifera
Part used: leaves
The antioxidants polyphenols myricetin and kaempferol have been correlated with neuroprotective properties
Effective in inhibiting cytochrome P-450 activity (3A4)

Anxiety and Insomnia

Anxiety is a mental disorder characterized by excessive fear and distress
Neurobiological mechanism of anxiety is related to dysregulation of serotonergic, noradrenergic, glutamatergic, and GABA-ergic transmission
Insomnia is the most common sleep disorder, caused by abnormalities in various pathways, including GABA receptor, cortisol level, cytokines, circadian rhythm, and excitatory amino acid (glutamate and aspartate)

Kava

Scientific name: Piper methysticum
Constituents: kavalactone (dihydrokavain, methysticin)
Mechanism: selectively acts on limbic system, promoting anxiolysis without sedation
Drug-herb interaction: may potentiate effects of other anxiolytics and may counter the effects of dopamine, reducing the effectiveness of medications for Parkinson's
Contraindications: depression, liver disease, pregnancy, and lactation
Adverse effects: extended consumption of large doses may cause a scaly, yellowing skin condition and possible hepatotoxicity

Valerian

Scientific name: Valeriana officinalis
Part used: root
Constituents: volatile oil, valerenic acid (sesquiterpene), and the iridoid valepotriate constituents
Mechanism of action: allosterically modulates GABA-A receptors, related to valerenic acid
Standardized products: pharmaceutical products are mainly produced from aqueous or hydro-alcoholic extracts (70% ethanol, herb-to-extract ratio 4-7:1)
Adverse effects: unlike benzodiazepines, valerian appears to cause no residual morning sleepiness, but may slightly impair judgment and driving ability for two to three hours after intake
Drug interactions: may potentiate the sedative effects of barbiturates
Dosage: as a sleep aid, take a single dose of ½ to 1 hour before bedtime

Songha Night

The combined mechanism of action of the two extracts contained in Songha Night may induce a synergistic effect, acting on two targets, normalizing the hyperactive excitatory brain system and increasing GABA levels

Passion Flower

Scientific name: Passiflora incarnata
Constituents: flavonoids (chrysin)
Mechanism of action: chrysin binds to benzodiazepine receptors sites and acts as an agonist for GABA activity, accounting for passion flower's anxiolytic properties
Used in combination with valerian root and lemon balm for conditions of difficulty in falling asleep due to nervousness

Melatonin

The primary hormone of the pineal gland, secreted exclusively at night in both nocturnal and diurnal species
Melatonin secretion undergoes a predictable change over the life span, declining around the time of puberty
Mean circulating melatonin levels in aged individuals are significantly lower than in young healthy adults
The effect of melatonin on sleep is likely mediated via specific melatonin receptors, MT1 receptor subtype
Recommended dose: 1-3 mg/night for infants and preschool children, 2.5-5 mg/night for school-age children, and 1-5 mg/night in adolescents
Administration: 30-60 minutes before bedtime, treatment should not exceed 4 weeks
Research indicates melatonin exerts a sleep-promoting action by accelerating sleep initiation, improving sleep maintenance, and marginally altering sleep architecture
Drug interactions:
- Drugs that inhibit CYP1A2 can increase serum melatonin, including ciprofloxacin, erythromycin, and tricyclic antidepressants
- NSAIDs can suppress endogenous melatonin production, necessitating supplemental melatonin
- May interact with blood thinning agents, increasing the risk of bleeding

Ergotamine

An alkaloid extracted from ergot (Claviceps purpurea), a parasitic fungus that grows on cereals, usually rye
Used to treat severe migraine that cannot be controlled with other drugs, but can cause severe adverse reactions and there are restrictions as to the maximum daily and weekly doses
Not suitable for children

Feverfew

Scientific name: Tanacetum parthenium
Constituents: parthenolide
Prophylaxis and treatment of migraine
Appears to work best in classic migraine with sensitivity to light
The antimigraine activity of feverfew is due to its prostaglandin inhibition
Numerous double-blind trials have been conducted, with three meta-analyses concluding that feverfew extracts are superior to placebo for decreasing the frequency and severity of migraine headaches
No serious side effects have been reported, but women who are pregnant should not use feverfew as it may cause the uterus to contract, increasing the risk of miscarriage or premature delivery

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Description

This quiz covers the central nervous system, including its effects on various diseases and disorders, and the role of plants in calming or stimulating the CNS.