Topic 3: Emetics, Dementia, Analgesic Flashcards
Emetic Response in the Brain
The emesis (vomiting) response is centered in the chemoreceptor trigger zone (CTZ) in the medulla of the brainstem.
Neurotransmitters that mediate the emetic response
dopamine and serotonin. mediate the emetic signals and motor reflexes in the stomach.
Ipecac (psychotria ipecacuanha)
Common name: ipecac, ipecacuanha, Brazil root
Geography: rainforest tree in Brazil
Ethnomedical Use: emetic, expectorant, intestinal amoebas
Active compounds: emetine, cephaeline, emetamine
Chemical Class:alkaloid
Chemical derivatives: dihydroemetine
Ipecac Mechanism of action
effect on the chemoreceptor trigger zone in the medulla of the brainstem.
local, direct irritation on the GI tract
Ipecac modern medical uses
emetine and dihyroemetine:
emetic- vomiting
amoebicide ( treats entamoeba histolytica)
Alzheimer’s Dementia histopathology
death and disappearance of nerve cells in cerebral cortex.
Clusters of thickened neuritic plaques are seen in the brain cortex.
suspected association with free radical mediated excessive lipid peroxidation & cell damage.
Alzheimer’s Dementia clincal (symptoms, etc. )
- most common cause of dementia in the elderly.
- most important neurological degenerative disease
- usually develops gradually over 10 or more years
- memory loss
- psychiatric disturbances e.g. depression, delusions, hallucination
- patient may eventually loose the ability to move, think and speak
Oxidation
to cause an element or radical to combine with oxygen or to lose electrons.
free radicals
molecules with the power to oxidize. They are oxidants.
Free radical scavengers
endogenous or exogenous molecules that chemically neutralize the oxidative effects of free radicals. Are antioxidants
Molecules that reduce dementia
ginkgo biloba leafy green vegetables blueberries (berries in general) caffeine Omega-3 fatty acids (walnuts, hemp seeds, flax seeds, kiwi, fruit, salmon) folic acid (oranges, spinach) Vitamin E Rivastigmine curcumin cannabis sativa
Ginkgo Biloba
Common name: ginkgo
Geography: tree native to China, cultivated all over today
Ethnomedical Use: senility, recovery from stroke, enhancement of mental functioning, brain ‘tonic’, enhance blood supply to whole body, treats peripheral vascular disease
Active compounds: ginkgolides, terpenoids (organic acids)
Ginkgo Mechanism of Action
- enhance cerebral and general body circulation.
- free radical scavengers (antioxidants) that inhibit lipid peroxide formation and cell damage.(flavanoids and terpenoids)
Ginkgo Modern medical uses
- Alzheimer’s
- senitlity
- enhancement of mental functioning
- peripheral vascular disease
Blueberries
Vaccinium corymbosum- originiated in E. USA
Vaccinium angustifolium- originated in N.E. North America
help reduce the development of Alzheimer’s disease
Caffeine and Dementia
Reduces development of dementia by blockade of adenosine receptors in the brain.
Caffeine Sources
coffee robusta- coffee
camellia sinesis- tea
theobroma cacoa- chocolate
cola acuminata- cola nut
curcumin (tumeric)
Curcuma longa Geography: India Ethnomedical Use: cooking, topically to treat infections and to enhance brain functioning Active compounds: curcumin Chemical Class: polyphenolic molecule
Rivastigmine
- Derived from physostigmine
- used to treat Alzheimer’s
- Seed from Physostigmus veneosum
- inhibits acetylcholinesterase which results in increased levels of acetylcholine in the CNS
- taken as a pill or skin patch
Cannabis Sativa
Common name: marijuana
Geography: Asia, open sunlight
Ethnomedical Use: used for 1000s of years for anti inflammatory, analgesic, anticonvulsant, antidepressant, nausea, anti emetic, appetite stimulant, glaucoma
Active compounds: THC
Cannabis Sativa
Common name: marijuana
Geography: Asia, open sunlight
Ethnomedical Use: used for 1000s of years for anti inflammatory, analgesic, anticonvulsant, antidepressant, nausea, anti emetic, appetite stimulant, glaucoma
Active compounds: THC
Cannabis Sativa and Dementia
Reduction in the development of memory loss and other symptoms of Alzheimer’s
Cannabis Sativa and Dementia
Reduction in the development of memory loss and other symptoms of Alzheimer’s
THC
tetrahydrocannabinol
marinol and dronabinol are pharmaceuticals derived from THC and nabilone is a chemical derivative.
THC
tetrahydrocannabinol
marinol and dronabinol are pharmaceuticals derived from THC and nabilone is a chemical derivative.
Therapeutic Benefits of THC
ease moderate pain and is neuroprotective which can reduce the risk of dementia.
Therapeutic Benefits of THC
ease moderate pain and is neuroprotective which can reduce the risk of dementia.
Cannabidiol (CBD)
- from cannabis sativa
- treats anxiety, seizures, and nausea
- major constituent of the plant aside from THC
Cannabidiol (CBD)
- from cannabis sativa
- treats anxiety, seizures, and nausea
- major constituent of the plant aside from THC
Cannabinoid receptors
CB1: central. brain cortex, hippocanthus, striatum and cerebellum
CB2: peripheral.
exogenous THC has nearly the same effect on both.
Cannabinoid receptors
CB1: central. brain cortex, hippocanthus, striatum and cerebellum
CB2: peripheral.
exogenous THC has nearly the same effect on both.
Endogenous cannabinoid molecules
anadamide- a brain lipid, binds to CB1 and is derived from arachidonic acid
palmitylethanolamide- binds to CB2
Endogenous cannabinoid molecules
anadamide- a brain lipid, binds to CB1 and is derived from arachidonic acid
palmitylethanolamide- binds to CB2
Cannabis Sativa Therapeutic uses
anti nausea anti emetic appetite stimulant analgesic glaucoma muscle relaxant anti convulsant
Cannabis Sativa Therapeutic uses
anti nausea anti emetic appetite stimulant analgesic glaucoma muscle relaxant anti convulsant
Chocolate (theobroma cacao)
contains three unsaturated N-acylethanolamine lipids:
N-oleoyethanolamine
N-linoleoylethanolamine
Anandamide
The first two inhibit anandamide hydrolysis.
All three may mimic cannabinoids by activating the receptors or increasing anandamide levels.
Chocolate (theobroma cacao)
contains three unsaturated N-acylethanolamine lipids:
N-oleoyethanolamine
N-linoleoylethanolamine
Anandamide
The first two inhibit anandamide hydrolysis.
All three may mimic cannabinoids by activating the receptors or increasing anandamide levels.
Papaver Sominoferum (opium)
Common name: opium
Geography: W. Mediterranean & Near East
Ethnomedical Use: analgesic, inebriate, hypnotic, diarrhea, cough
Papaver somniferum botanical extracts
tincture of opium
paregoric of opium (opium with camphor oil, anise oil and benzoic acid)
Opium active compounds
- 20 alkaloids
- morphine, morphine sulfate, morphine HCl
- codeine, codeine sulfate, codeine phosphate
- thebaine
- narceine
- papverine
Opium chemical derivatives
morphine–> heroine
thebaine–> naloxone
papaverine–> verapamil
Morphine derivatives
codeine
heroin
dihydromorphone
hydromorphone
Thebaine derivatives
naloxone
hydrocodone (vicodin)
oxycontin
synthetic opiates
meperidine- fast acting
proproxyphene
fentanyl- 100x more potent than morphine, fast acting, short half life
methadone- weak agonist which is taken orally to treat people who are opiate addicts.
Papaver sominferum mechanism of action
inhibition of the release of substance P– is associated with the relief of pain
Endogenous opiates
opiopeptins; including beta-endorphins and enkephalins which bind to the same receptors as morphine (opiate receptors) and other exogenous opiates
Papaver Sominferum (opium) Uses
morphine: analgesic
Codeine: analgesic, anti tussive (codeine can be metabolized into morphine)
noscapine: anti tussive (cough)
naloxone: treats morphine overdose. agonist that binds to receptors and outcompetes the binding of stronger agonists, resulting in an antagonistic effect.
papaverine: vasodilator, smooth muscle relaxant.
verapamil: vasodilator, treats hypertension and tachyarrhythmia
Opiate Addiction and dopamine
There is evidence for interaction between opioids and dopamine pathways through stimulation of nucleus accumbens in the dopamine pathway.
This mediates opioid-induced reward and addiction.
demorphine
derived from secretions off the back of South American frogs.
Natural hepta-peptide that is a natural opioid with high potency(30-40x more potent than morphine) and selectivity to mu opioid receptors.
Less likely to produce drug tolerance and addiction
