Tuesday, January 6, 2009

depressants- continued

Antianxiety drugs
" minors" : this term is used to distinguished from the " major tranquilizers"
compounds such as chlorpromazine( Thorazine) which is used to manage psychosis

The first minor tranquilizer is meprobamate( Miltown/ Equanil)
The most popular appeared in 1960s: benzodiazepines: 
  • chlordiazepoxide( Librium)
  • diazepam( Valium)
  • triazolam( Halcion)
  • alprazolam( Xanax)
  • lorazepam( Ativan)
  • temazepam( Restoril)
  • clonazepam( Klonopin)
compared with barbiturates, benzodiazepines are safere in overdose and somewhat less dangerous in combination with alcohol

Flunitrazepam(Rohypnol) is a remedy for insomnia and pre-anesthtic medication for patients undergoing surgery. It is more potent and lasts longer than Valium. Availvale in the black market under the name " roofies". Users used this to enhance the effect of other drugs

It is very difficult to wean of benzodiazepines, since withdrawal is unpleasant and dangerous


GHB( Gammahydroxybutyrate)

GHB is an endogenous downer made in small amount in the brain as a metabolite of the sedatiuve neurotransmitter GABA
Synthetic GHB stimulates the pituitary gland to release growth hormone, which can help convert fat to muscle.

A teaspoon of GHB dissolved in warm water and taken on an empty stomach can cause the effect akin to alcohol and methaqualone intoxication

GHB can cause nausea and marked incoordination along with " hypersomnolence": a kind of temporary stupor in which people can stop breathing for periods.

GHB increases rather than suppresses dreaming. in this aspect, it is different from other depressants.

General Anesthetics:
gases or volatile liquids administered by inhalation through a mask placed over the face or tubes in the throat

Like all depressants, anesthetics can killby shutting down the respiratory centre and other vital functions.

CHroroform is the oldest form, but it is toxic so it is no longer used

Ether/ Diethyl ether : is still used before surgery.  But it can be explosive from accidental sparks or flames..

Nitrous oxide only has a faint odor, non toxic and nonflammable. does not produce complete loss of consciousness . Often used by dentistry orminor surgery

Some people havetried to get nitrous oxide directly from pressurized tanks, whipping cream. But people may get frostbites of the nose and the mouths of they attemptto do it incorrectly. Asphyxiation by breathing straight from face mask( without any supply of oxygen) may causedeath.

Narcotics
narcotics are drugs that produce stupor( state of reduced sensitivity) by depressing brain function, but their depressant function is different from sedative-hypnotics or general anesthetics

The parent of all narcotics is opium, a dark gummy solid made from opium poppy. As the flower wither, the green pods, which contain many tiny seeds, begin to ripen and swell. If the pods are ripened fully, they turn brown and dry. While still unripe, the pods contain a milky juice that can becollected by letting it ooze from the knife cuts. When dried, this ooze is crude opium.

Many oral preparations of opium were made in the past. Two that survive into our own time are paregoric, a dilute tincture ofopium cimbined with camphor, and a deodorized tincture ofopium, formerly known as laudanum

Crude opium is very bitter and contains more than twenty different drugs, of which the most important is morphine.

In 1803, morphine is prepared as a soluble white soluble poweder that can be mixed with water for injection

Codeine( methylmorphine) is another natural constituent of opium. More active by mouth than other narcotics, is a weaker pain reliever than morphine and doctors frequently prescribe it to treat moderate pain.

Heroin( diacetyl morphine) is more potent than morphine: producing the same effect in smaller dose.

Drugs derived from morphine and other opium compounds are opiates. Demerol( purely synthetic). In general, all opiates produce the same effect, only differ in their potency.

these generally act on the brain and bowel. THese paralyze the bowel, so narcotics can be used to treat diarrhea. Prolonged use induces chronic constiapation.

Tolerance for addictive dose of sedatives-hypnotics develop faster than their lethal dose- making them more easily overdose- compared to that of narcotics. Heroin overdose death is more often due to poor control of the drug.
Intravenous heroin use is most addictive due to its high potency and short duration

oxycodone: a semisynthetic opiate: blended with aspirin as Percodan and with acetaminophen as Percocet
Oxycotin: a more potent and time released version ofoxucodone.

methadone is a form of heroin maintenance. It blocks the effect of heroin, so gives junkies little motivation to shoot heroin. Oral methadone is an addicting narcotic but gives little euphoria.

A new semisynthetic opiate is called  buprenorphine has beenused for heroin addiction. It blocks the high of heroin and can be given in higher doses without suppressing breathing.
 

depressants

lower energy level of the nervous system, reducing sensitivity to outside stimulation and, in high doses, inducing sleep.
types:
Sedative-hypnotics : alcohol, sleeping pills and anti anxiety drugs

Alcohol= ethyl alcohol, ethanol
Production of alcohol depends on yeast, which feeds on sugar, making alcohol and Carbon dioxide as by products.
To grow and multiply, yeast cells need water, warmth, sugar.
At high doses, alcohol is a poison that kills the yeast that makes it as well.

Natural sources of sugar available were fruits and honey
Starch may be a source of sugar as well. But enzymes must contain starch into sugar first.
In standard beer making, sprouted barley( malt) is used to convert the starch of grain into sugar so that yeast cam grow.

Distilled alcohol is made by heating wine and cooling and condensing the vapors into another container. This process increases the content of alcohol from 40 to 50 percent

Scotch abd bourbon whiskeys are made from beerlike preparation of grain
Rum is distilled from fermented molasses
vodka is diluted ethyl alcohol, so is gin

The stronger the drink, the faster the blood concentration level rises
As with many other psychotic drugs, the mood onset depends on the situation.

As alcohol concentration increases, it depresses more and more of the nervous system, producing familiar symptoms of drunkenness. People become drunk in very different ways, depending on theirpersonalitites

DEPENDENCE: is a serious matter: marked by extreme craving, tolerance and withdrawal.  Delirium tremens( the DTs) is the worst form of withdrawal, may even cause death, which is worse than narcotics.
cirrhosis of the liver, loss of sexual potency, inability to digest food are someof the problems

barbiturates and other sleeping pills " downers"

the first barbiturates= barbital 
2nd one= phenobarbital appeared in 1912
These two are long acting barbiturates because their effects last for 12 to 24 hours. day time sedatives and nighttime hypnotics. these don't cause high, so few people take them to get high.


Short acting:
last 6-7 hours
amobarbital (Amytal)
pentobarbital( Nembutal)
hexobarbital( Sombulex)
secobarbital( Seconal)
These behave liek alcohol. 

Very short acting, injection produces immediate unconsciousness
Thiopental( Pentothal) : used as anesthetic for surgical operations

Tolerance for downers on mood are faster than the tolerance for lethal dose. Thus, higher risk of overdose on sleeping pills.
Because their depressant effects are additive, combining alcohol and downers and dangerous.

Some people like to combine downers and stimulants: 
Dexamyl( mixture of amobarbital and dextroamphetamine(Dexedrine))

There area number of nonbarbiturate downers: methaqualone being the most popular ( marketed under brands like : Quaalude, Sopor and Mandrax), less likely to depress the respiratory system, but still there have been reports of death by combining alcohol and methaqualone

Another downer: chloral hydrate  : is the oldest sleeping drug still in medical use. 
Slipped into alcoholic drinks " Mickey Finn" or " knock out drops" used to drug unsuspecting people for kidnapping or robbing them.

Other nonbarbiturate downers include : glutethimide( Doriden), methyprylon (Noludar), ethchlorvynol( Placidyl) and paradehyde. All of these drugs are used as hypnotics.

The most popular downer today is zolpidem( Ambien)

Kinds of Stimulants

Coffee and Caffeine-containing plants
  • coffee strong stimulant
  • may cause shakiness, headaches 
  • will cause dependence

Tea containing L-theanine which causes " alert relaxation"
National drink of Brazil= guarana ( marketed as Zoom and Zing/ containining more caffeine than coffee)
Argentina: mate : from leaves of holly plants
chocolate: from cacao tree, its seeds are cocao beans, fat is cacoa butter, theobromine

Coca and Cocaine
not related to cocao/cocoa

Coca contains 14 drugs, most important of which is cocaine. Coca is a shrub, native to the hot, humid Andes.
Coca users put dried leaces in their mouth and work them into a large wad. They suck on the wad for thirty minutes, and spit out the residue. Must add a bit of alkali( lime) to enhance the effect

Coca contains 0.5 % of cocaine. While refined cocaine is 60% of drug. Snorting powder cocaine irritates the nose, smoking crack is bad for the lung. THe effect is short : 15 to 30 min. After which the users feel sluggish and unhappy

highly addictive such as that of cigarettes.

Amphetamines and related drugsr
synthetic drugs

structures resemble adrenalines and noagrenaline
effect resemble cocaine but longer lasting= 4 hours
more toxic than cocaine because the liver cannot detoxify effectively
types:
  1. Plain amphetamines( Benzedrine)
  2. Dextroamphetamine( Dexedrine)
  3. methamphetamine(Methedrine)
  4. methylphenidate( Ritalin)
  5. modafinil( Provigil)
  6. Adderall(combination of dextroamphetamine and methamphetamine) used for ADHD
explosive growthof methaphetamine: meth, crank. crystalline, smokable form= " ice", " crystal"
hazardous: smoking and injecting

Look-alike drugs:
caffeine 
ephdrine: produces more anxiety and less euphoria than meth
phenylpropanolamine(PPA): used to be in nasal decongestants
synephrine

Tobacco and Nicotine
most dangerous
tolerance for its toxicity develops in the matters of hours( whereas days or weeks for heroin and months for alcohol)

most addictive in the form of cigarrettes, equivalent to crack cocaine and ice
Smokers from cigarettes delivers concentrated nicotine to vital brain centres within a few seconds- faster than heroin injection reaching the brain.




Stimulants

Most common stimulant neurotransmitter= noradrenaline/ norepinephrine which is an endogenous chemical which structure resembles that of hormone adrenaline produced by adrenal gland

Stimulant drugs work by causing nerve fibres to release noreadrenaline and other stimulating neurotransmitters. End result= release of more stimulating neurotransmitters

It makes people feel wakeful alert and often happy

heart beats faster, blood pressure rise.
fingertips and tips ofnose becomes cold

laxative effect

some of these effects are mediated by the sympathetic system( chemical messenger= noradrenaline) which cause the adrenaline secretion by adrenal gland.



pharmacology

Endogenous: endorphins, norephedrine, ephedrine
Natural drugs
  • crude forms: resin of Viola tree, cocaine from coca tree
  • refined forms: morphine, cocaine, mescaline
Semi synthetic drugs:
2 acetic acid groups to morphine ==> heroin
LSD (lysergic acid diethylaminde) == from lysergic acid( toxic)  from a ergot fungus

Synthetic drugs:
Valium
PCP( Phencyclidine)
Secobarbital( Seconal)