Analgesics Flashcards
Analgesic drug (painkillers)
substances relive pain by exerting depressing action on the central nervous system
Narcotic drug
analgesic or pain killing substance that depress vital body function such as blood pressure, pulse rate and breathing rate. Now also commonly used for any socially unaccepted drugs
Morphine, codeine heroin and methadone
Morphine, codeine, heroin, methadone all have analgesic property.
Also called opioids.
Morphine, codeine, heroin have the same origin.
Methadone has a very different origin.
Morphine and codeine are alkaloids.
Opium
- The dried milky juice of unripe seedpods of the opium poppy.
The chief constituents of opium are the alkaloids codeine and morphine from which heroin is synthesised.
Those constitutes are classified as opium alkaloids.
Harvesting opium
- Tapping the pod (cutting). Can’t be too deep or shallower. Can be done more than once
- Tapping normally done in the later afternoon
- The secretion of opium can take few days
- The blackened opium was scraped off the pot
- In average 50 milligrams crude opium per pod
Anatomy of opium poppy
- The skin of the poppy pod encloses the wall of the pod ovary. The ovary wall consists of an outer, middle and inner layer
- The plants latex is produced within the ovary wall and drains into the middle layer
- The cells of the middle layer secrete more than 95% of the opium when the pod is scored and harvested
Alkaloids
Alkaloids are natural products contain one or more nitrogen atom and are therefore basic in character.
other alkaloids
- Tropane alkaloids such as atropine
- Quinoine alkaloids such as quinine
- Isoquinoline alkaloids such as morphine
- Purine alkaloids such as morphine
- Purine alkaloids such as caffeine
Opiods
term used to refer to any drug with an opium like action,
All opioid drugs have similar effects. At low doses they relieve pain and anxiety, and if the does is increased, they produce a sedative effect.
- Opioids give the classical model of addiction- a primary chronic neurobiological disease
- Addictive drugs stimulate pleasure and motivation pathways in the brain
- repeated exposure to these drugs can fool the brain into prioritising drug
- Opioids produce tolerance
- Stopping after repeated use produces withdrawal
Opium nad heroin timeline
- 1300 B.C Egyptians started to cultivate opium poppies for self use and trade
- 1000 A.D The medical use of opium poppy seeds is widespread
- 1803 Morphine isolated from poppies by a German pharmacist
- 1874 – Heroin is first synthesized from morphine by a chemist
- 1911– British Pharmaceutical Codex notes that heroin is as addictive as morphine.
Morphine
- Isolated from the juice obtained from unripe seed pods of the opium poppy, morphine is one of the most effective painkillers known
- Class A
- It is a potent analgesic, and its primary clinical use is in the management of severe pain.
- highly addictive and the body builds up a tolerance quickly
- administered by several routes
Codeine
- Codeine is found in small concentration
- most codeine used in medical products is synthesized from morphine
- Class B
- moderate to low, potency and dependency compared to morphine
Heroin I (diamorphine)
Heroin is the di-ester of morphine
made from morphine via chemical reaction for medical or illegal use
It is unavailable from opium poppy therefore it’s not a alkaloid
Colour affected by diluent constituents
Some sample may smell of acetic acid
It can be smoked snorted or dissolved in water and injected
Also known as brown, skag, H, horse, gear, smack
Class A
Heroin is a white powder when its pure. But street heroin can be anything from off white to brown powder and black tar or granular lump
Morphine codeine heroin chemistry I
Alcohol group (OH) (polar groups can form hydrogen bonding)
Ether group (C-O-C) (less polar than OH group, stable)
Amine group (C-NH-C, less polar has basic property)
Ester group (less polar than OH, less stable than ether
Carbon bonding (valency of 4, tetrahedral in shape)
Amine bonding (valency of 4, distorted tetrahedral, pyramid, in shape) Oxygen (valency 2)
Chiral carbon (all four substitution on carbon are different)
Country origin
◦ South East Asia – Thailand, Myanmar (Golden Triangle)
Associated with white type heroin hydrochloride of high purity
◦ South Western Asia – Afghanistan, Pakistan etc. (Golden Crescent)
Associated with brown type heroin often base
~87% of the world’s heroin is derived from Afghanistan
◦ South America – Mexico etc.
Associated with black tar heroin
Poorly acetylated
Important for profiling of market drugs