All Drug's Pharmacokinetics Flashcards
Caffeine: about
religious drinks
- tea (china)
- coffee (ethiopia)
Caffeine: membranes
- simple diffusion to cross membranes and BBB
Caffeine: toxicity
- LD50 = 150 to 200 mg/kg BM
Caffeine: absorption
- RoA = ingestion
- absorbed by the stomach and small intestines within 45 mins of consumption
Caffeine: half life
t1/2 = approx 3 to 4 hours
Caffeine: metabolism
metabolised in liver by CYP450 enzyme system
Caffeine: metabolites
- paraxanthine
- theobromine
Caffeine: elimination
primarily eliminated through the kidneys and excreted through urine
Caffeine: potential for abuse and addiction
- very dependence-producing
- withdrawal effects caused by adenosine receptor density, and therefore adenosine sensitivity (depression, fatigue, irritability, headaches)
Nicotine: about
- alkaloid, organic compound from tobacco plant
- lipophilic free base
Nicotine: membranes
- simple diffusion to cross membranes and BBB
- environment pH affects its absorption (small intestine, not stomach)
Nicotine: toxicity
- cancer (90% of all lung cancers)
- COPD, asthma, emphysema
- LD50 = 30 to 60mg
Nicotine: absorption
- RoA = inhalation, ingestion, buccal, transdermal
- inhalation = most addictive
- transdermal = least addictive because of low dose and speed of delivery to the brain
Nicotine: half life
t1/2 = approx 2 hours
Nicotine: metabolism
metabolised in the lungs, kidneys, and liver by CYP450 and aldehyde oxidase enzyme systems
Nicotine: metabolites
cotinine (t1/2 = approx 16 hours)
Nicotine: elimination
primarily eliminated through the kidneys and excreted through urine
Nicotine: potential for abuse and addiction
- very dependence-producing (used as stress relief, weight control, social factor)
- withdrawal: irritability, anxiety, excessive hunger (blood sugar drop)
Alcohol (ethanol): about
fermentation of sugars, anaerobic respiration by yeast - changes the sugars into ethanol and carbon dioxide
Alcohol (ethanol): membranes
- simple diffusion to cross membranes and BBB
Alcohol (ethanol): absorption
- approx 80% absorption from upper intestine
- total absorption is unaffected by food in stomach
- avg vol of distribution is 0.54 l/kg
Alcohol (ethanol): half life
t1/2 = approx 3 to 5 hours but can vary
Alcohol (ethanol): metabolism
95% of alcohol is metabolized by alcohol dehydrogenase enzyme in the liver
Alcohol (ethanol): metabolites
- acetaldehyde first, broken down to acetate
Alcohol (ethanol): elimination
- liver (90%), and urine, sweat and breath
Alcohol (ethanol): potential for abuse and addiction
high potential for abuse based on its action in the glutamtergic, GABAergic, dopaminergic, and serotinergic systems
- withdrawal: tremors, irritability, nausea, anxiety, depression
Cocaine: about
- alkaloid
- from coca plant
Cocaine: membranes
- passive diffusion accross membranes and BBB
Cocaine: human health
chronic use: cardiovascular issues due to vasoconstriction
Cocaine: absorption
- RoA = ingestion, inhalation, IV, intranasal
- primarily absorbed through mucous membranes
Cocaine: half life
t1/2 = approx 15 to 90 mins
Cocaine: metabolism
- minimal liver metabolism (CYP450)
Cocaine: metabolites
- norcocaine
- benzoylecgonine
Cocaine: elimination
primarily eliminated through the kidneys and excreted through urine
Cocaine: potential for abuse and addiction
- potential for both physical and psychological dependence
- short half life (need for frequent dosing)
- withdrawal: tremors, irritability, nausea, anxiety, depression
Amphetamines and methamphetamines: membranes
- passive diffusion accross membranes and BBB
Amphetamines and methamphetamines: absorption
- RoA = ingestion, intranasal, inhalation, intravenous, intramuscular
Amphetamines and methamphetamines: half life
methamphetamines: t1/2 = approx 10 to 12 hours
amphetamines: t1/2 = approx 4 to 6 hours
Amphetamines and methamphetamines: metabolism
metabolised by the liver by the CYP450 enzyme system
Amphetamines and methamphetamines: metabolites
amphetamine
Amphetamines and methamphetamines: elimination
primarily eliminated through the kidneys and excreted through urine
Amphetamines and methamphetamines: potential for abuse and addiction
- potential for both physical and psychological dependence
- withdrawal: tremors, irritability, nausea, anxiety, depression
LSD: about
- ergot fungus
-1960s
LSD: membranes
- passive diffusion accross membranes and BBB
LSD: absorption
- RoA = ingestion, sublingual, transdermal
- completely absorbed in the GI tract (oral)
LSD: half life
t1/2 = approx 2.5 hours
LSD: metabolism
- in the liver by CYP2D6, CYP2E1, CYP3A4
LSD: elimination
primarily eliminated through the kidneys and excreted through urine
LSD: potential for abuse and addiction
- low potential for abuse and physical dependencevery low tolerance can occur
Ketamine: about
- dissociative anaesthetic
- originally used for veterinary purposes
Ketamine: membranes
- passive diffusion accross membranes and BBB
Ketamine: absorption
- RoA = ingestion, intranasal, intravenous, intramuscular
Ketamine: half life
t1/2 = approx 2 to 3 hours
Ketamine: metabolism
metabolised in the liver by CYP450 enzyme system
Ketamine: metabolites
norketamine (active drug)
Ketamine: elimination
primarily eliminated through the kidneys and excreted through urine
Ketamine: potential for abuse and addiction
- potential for both physical and psychological dependence
- withdrawal: tremors, irritability, nausea, anxiety, depression
Heroin: about
- opioid derived from morphine
Heroin: membranes
- passive diffusion accross membranes and BBB
Heroin: absorption
- RoA = intravenous, intramuscular, inhalation, intranasal
Heroin: half life
t1/2 = approx 2 to 6 mins
Heroin: metabolism
metabolised in the liver through hydrolysis using acetylcholinesterase enzymes
Heroin: metabolites
morphine
Heroin: elimination
primarily eliminated through the kidneys and excreted through urine
Heroin: potential for abuse and addiction
- potential for both physical and psychological dependence
- short half life (need for frequent dosing)
- withdrawal: tremors, irritability, nausea, anxiety, depression
Marijuana: about
from the cannabis plant
Marijuana: membranes
- simple diffusion accross membranes and BBB
Marijuana: absorption
- RoA = inhalation, ingestion, transdermal, sublingual
Marijuana: half life
t1/2 = approx 18 to 20 hours
Marijuana: metabolism
metabolised in the liver mainly by CYP450 enzymes
Marijuana: elimination
primarily eliminated through the liver/bile and excreted through faeces but also eliminated through the kidneys and excreted through urine
Marijuana: potential for abuse and addiction
low potential for physical dependence, high potential for psychological dependence for frequent use