Showing posts with label Central Nervous System. Show all posts
Showing posts with label Central Nervous System. Show all posts

Monday, June 22, 2020

Codeine, CYP2D6 phenotypes and morphine

Codeine is metabolised to morphine by CYP2D6.
CYD2D6 displays huge variation in activity due to genetic polymorphism.


4 phenotypes of expression are identified depending on the level of activity
  • UMs: Ultrarapid metabolisers
  • EMs: Extensive metabolisers (Most Common)
  • IMs: Intermediate metabolisers
  • PMs: Poor metabolisers
Morphine is formed at a very fast pace in ultrarapid metabolisers.
In adults with ultra rapid metabolisation: if codeine is administered at therapeutic doses then resulting levels of morphine is unlikely to cause respiratory depression. But the possibility increases substantially in overdosage.
In lactating mothers with ultra rapid metabolisation: codeine administered at therapeutic doses may result in high levels of morphine in milk; there are case reports of respiratory depression occurring in infants of such mothers.

Monday, November 28, 2016

Central nervous system classification

Antidepressants 
Anti-anxiety drugs 
Antipsychotic drugs 
Antimanic drugs
Antiepileptic drugs
Anti Parkinsonian drugs 
Sedatives and hypnotics
General anaesthetics 
Opioids
CNS stimulants 
Cerebroactive drugs 
Psychotomimetics 
Antiaddictives

Antiaddictives classification


1) Alcohol deaddiction

Disulfiram
Naltrexone
Acamprosate


2) Nicotine deaddiction
Nicotine replacement therapy

Inhaler
Spray
Gum
Lozenges
Transdermal patch


3) Opioid deaddiction

Methadone
Clonidine
Buprenorphine
Buprenorphine-naloxone

Psychotomimetics classification


1) Cannabinoids
Tetrahydrocannabinol (Cannabis indica derived)

Bhang
Majoon
Charas
Ganja

2) Indole Amines

Lysergic acid dimethylamide
Lysergic acid amide
Psilocybin
Harmine
Bufotenin

3) Phenylalkyl Amines

Mescaline
Dimethoxyamphetamine

4) Aryl cyclohexyl Amines
Phencyclidine

Cerebroactive drugs classifiaction


1) Cognition Enhancer
Piracetam

2) Cholinergic Activators

Tacrine
Rivastigmine
Donepezil
Galantamine

3) Metabolic Enhancers

Dihydroergotoxine (Codergocrine)
Nicergoline
Piribedil

4) Vasoactive Cerebral Protector

Pyritinol (Pyrithioxine)
Ginkgo biloba

5) NMDA antagonist
Memantine

CNS stimulants classification


1) Respiratory stimulants (Analeptics)

Doxapram
Prethcamide

2) Convulsants

Picrotoxin
Pentylenetetrazol (PTZ)
Strychnine
Bicuculline

3) Psychomotorstimulants

Amphetamines
Methylphenidate
Pemoline
Cocaine
Caffeine

4) Other Drugs Causing Reflex CNS Stimulation

Lobeline
Nicotine
Veratrum
Ammonia

Opioids classification


Based on source

1) Natural Opium Alkaloids
a) Phenanthrenes

Morphine
Codeine
Thebaine

b) Benzoisoquinolines (non analgesic)

Papaverine
Noscapine

2) Semisynthetic opiates

Diacetylmorphine
Ethylmorphine
Pholcodeine

3) Synthetic opioids

Pethidine
Methadone
Fentanyl
Tramadol
Levorphanol
Ethoheptazine
Dextropropoxyphene


Based on mode of action

1) Pure Agonists

Morphine
Fentanyl

2) Partial μ Agonists

Buprenorphine
Propiram

3) Agonist- Antagonists

Butorphanol
Pentazocine
Nalbuphine
Nalorphine

4) Pure competitive Antagonists

Naloxone
Naltrexone 
Nalmefene

General anaesthetics classification


1) Inhalational Anaesthetics
a) Gases

Nitrous oxide;
Cyclopropane (no longer used)

b) Volatile liquids
i) Non-halogenated

Ether
Xenon

ii) Halogenated

Halothane
Sevoflurane
Isoflurane
Enflurane
Desflurane
Ethyl chloride

Chloroform (no longer used)
2) Intravenous (Non-volatile) Anaesthetics
a) Inducing agents (short acting):

Thiopentone
Methohexitone
Propofol
Etomidate
Ketamine

b) Slower acting drugs
i) Benzodiazepines

Diazepam
Lorazepam
Midazolam

ii) Steroid

Althesin
Pregnendone

iii) Opioid analgesia
Fentanyl

Sedatives and hypnotics classification


1) Barbiturates
a) Ultra short Acting

Thiopentone
Methohexitone
Hexobarbitone

b) Short acting

Secobarbitone
Butobarbitone
Pentobarbitone

c) Long acting

Phenobarbitone
Mephobarbitone


2) Benzodiazepines (BZD)
a)Hypnotics

Diazepam
Flurazepam
Nitrazepam
Flunitrazepam
Temazepam
Triazolam
Midazolam

b) Anti-anxiety drugs

Diazepam
Lorazepam
Alprazolam
Oxazepam
Chlordiazepoxide

c) Anti-convulsants

Diazepam
Clonazepam
Clobazam


(Flumazenil is a Benzodiazepine antagonist)

3) Non-BZD Hypnotics

Zaleplon
Zopiclone
Eszopiclone
Zolpidem


4) Miscellaneous (no longer used)

Chloral hydrate
Meprobamate
Paraldehyde
Glutethimide