Transcript Drugs Classification

Drugs Classification
Drugs Administration
and Absorption
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Ingestion
 Dissolve in the stomach & absorbed by intestine
 Absorbed thought stomach walls (e.g., alcohol)
 Absorption will depend on various factors:
 amount and type of food
Injection
 Strong, fast, predictable
 Subcutaneous, intramuscular, intravenous
Inhalation
 Difficult to regulate doses
Insufflation (snore)
 Absorption through mucous membrane of:
 nose, mouth, rectum, vagina
Psychoactive/Psychotropic Drugs
Action on Central Nervous System (CNS)
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Analgesics
Anesthetics
Anxiolytics (anti-anxiety agents)
Antidepressants
Antipsychotics
Anticonvulsants
Mood stabilizers
Stimulants
Depressants
Hallucinogens
Psychoactive Substances Usage
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Analgesics (painkillers)
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Psychiatric medications
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use in the treatment of psychiatric conditions
anxiolytics, antidepressants, antipsychotics, anticonvulsants,
and mood stabilizers
Recreational drugs
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used to relive pain without producing anesthesia or loss of
consciousness
used/abused for their mood and perception altering effects,
including those with accepted uses in medicine and psychiatry
frequently used include narcotics, stimulants, depressants,
hallucinogens
Entheogens
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used for ritual and spiritual practice, such as the mescalinecontaining peyote cactus or psilocybin-containing mushrooms
Psychoactive Drugs
Classification
Depressants
Stimulants
Narcotics
Hallucinogens
CNS Depressants
Slows down the central nervous system
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Provide feeling of relaxation
Reduced inhibitions
Impair reflexes
Impair coordination
Reduce reaction time
Slurring speech, stumbling walk, and loss of balance
Hand-eye coordination is reduced
Thought and judgment impaired
CNS Depressants
 Sedative
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Barbiturates
Benzodiazepines
Solvents-sedatives
Herbal sedatives
Nonbenzodiazepine
Uncategorized sedative-hypnotics
 Narcotics (opiate derivatives)
 Antihistamines (diphenhydramine)
CNS Depresants
Sedatives
 Also known as sedative-hypnotic
 Produces feelings of calmness, relaxation, sleepiness,
slowed breathing, reduction of anxiety, and at higher
doses slurred speech, staggering gait, poor judgment,
and slowcertain reflexes.
 Whenused to induce sleep tend to be higher doses
than those used to relieve anxiety.
 May be referred to as tranquilizers, depressants,
anxiolytics, soporifics, and sleeping pills.
 Can be abused to produce an overly-calming effect
(alcohol being the most common sedating drug).
 At high doses many of these drugs can cause
unconsciousness and even death.
CNS Depressants
Barbiturates
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Effect range mild sedation to anesthesia.
Effective as anxiolytics, hypnotics and as anticonvulsants.
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Widely used in surgical anesthesia.
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Have addiction potential, both physical and psychological.
Dangerous in overdose.
Used for physician-assisted suicide (PAS), and in
combination with a muscle relaxant for capital punishment
by lethal injection.
Thiopental is an ultra-short acting barbiturate that is
marketed under the name Sodium Pentothal is sometimes
used as a "truth serum". When dissolved in water, it can be
swallowed or administered by intravenous injection. The
drug does not itself force people to tell the truth, but is
thought to decrease inhibitions, making subjects more likely
to be caught off guard when questioned.
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CNS Depressants
Barbiturates
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amobarbital (Amytal)
pentobarbital (Nembutal)
secobarbital (Seconal)
Phenobarbitol (Luminal)
CNS Depressants
Benzodiazepines
 Minor tranquilizers with varying properties.
 Slow down the CNS.
 Useful in treating anxiety, insomnia, agitation,
seizures, muscle spasms, and alcohol withdrawal.
 Also used before medical procedures such as
endoscopies and dental work.
 Recreational stimulant users often use
benzodiazepines as a means of "coming down"
 All have an addictive potential.
CNS Depressants
Benzodiazepines (minor tranquilizers)
alprazolam (Xanax)
bromazepam (Lexotan)
clonazepam (Klonopin)
diazepam (Valium)
estazolam (Prosom)
flunitrazepam (Rohypnol)
lorazepam (Ativan)
midazolam (Versed)
nitrazepam (Mogadon)
oxazepam (Serax)
triazolam (Halcion)
temazepam (Restoril, Normison, Planum, Tenox, and
Temaze)
 chlordiazepoxide (Librium)
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CNS Depressants
Solvents-Sedatives
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chloral hydrate (Noctec)
diethyl ether (Ether)
ethyl alcohol (alcoholic beverage)
methyl trichloride (Chloroform)
CNS Depressants
Alcohol
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Among the most abused drugs in our society.
Can be as potent as many other illegal drugs.
Can cause severe damage to a developing fetus.
Reduces sensitivity to pain.
Long-term effect can produce damage to liver, heart and
pancreas.
Linked to gastro intestinal problems, malnutrition, high
blood pressure, and lower resistance to disease.
Also linked to several types of cancer; including esophagus,
stomach, liver, pancreas and colon.
People often do not realize that they are becoming
dependent on alcohol.
Other CNS Depressants
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Herbal sedatives
 kava
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valerian
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eszopiclone (Lunesta)
zaleplon (Sonata)
zolpidem (Ambien)
zopiclone (Imovane, Zimovane)
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ethchlorvynol (Placidyl)
glutethimide (Doriden)
ketamine (Ketalar, Ketaset)
methaqualone (Sopor, Quaalude)
methyprylon (Noludar)
ramelteon (Rozerem)
Nonbenzodiazepine sedatives
Uncategorized sedative-hypnotics
Narcotics
 Refers to opium, opium derivatives, and their
semi-synthetic or fully synthetic substitutes.
 Most medical professionals prefer the more
precise term “opioid”, which refers to natural,
semi-synthetic and synthetic substances that
behave pharmacologically like morphine, the
primary active constituent of opium.
 Main use: pain relief and cough suppressant.
Four broad classes of Narcotics
(opioids)
 Endogenous Opioids
 produced naturally in the body (endorphins)
 Opium Alkaloids
 morphine (the first alkaloid isolated from opium)
 codeine
 Semi-synthetic Opioids
 heroin and oxycodone
 Fully Synthetic Opioids
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methadone and pethidine
Clinical use of Narcotics
(opioids)
 Opioids have been used to treat acute pain
 such as post-operative pain
 Used in palliative care to alleviate
 severe, chronic, disabling pain of terminal
conditions such as cancer
 In recent years there has been an
increased use of opioids in
 management chronic pain (transdermal patches)
Clinical use of Narcotics
(opioids)
 Cough
 (codeine and hydrocodone)
 Diarrhea
 (opium)
 Anxiety due to shortness of breath
(oxymorphone)
 Detoxification
 (methadone and buprenorphine )
Narcotics Classification
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Opium alkaloids
Phenanthrenes naturally occurring in opium:
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Codeine
Morphine
Thebaine
Oripavine
Preparations of mixed opium alkaloids, including papaveretum,
are still occasionally used.
Semisynthetic derivatives
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Diacetylmorphine (heroin)
Dihydrocodeine
Hydrocodone
Hydromorphone
Nicomorphine
Oxycodone
Oxymorphone
Examples of Narcotics
Opium
Codeine
Morphine
Heroin
Methadone
Oxycodone
Demerol
Dilaudid
Percodan
Lomotil
CNS Stimulants
Stimulate central nervous system (CNS)
Increase alertness and wakefulness
Some produce a sense of euphoria
Can be used therapeutically
 Narcolepsy - to counteract abnormal states that
diminish alertness or consciousness
 Used to boost endurance and productivity as well as
to suppress appetite
 Significant mood-altering effects
 Controlled substances in many jurisdictions
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Common Stimulants
Amphetamines
Methylphenidate
Methamphetamine
Methcathinone
Cocaine
Ecstasy
Stimulants
Amphetamine
 Also known as amfetamine, and benzedrine
 brand name: Adderall
 Prescription (Rx) stimulant used to treat
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ADHD
Traumatic brain injury
Narcolepsy
Chronic fatigue syndrome
Initially used to control appetite
 Also used illegally as
 a recreational club drug
 as a performance enhancer
Stimulants
Methylphenidate (MPH)
 Amphetamine-like Rx stimulant
 Used to treat
 ADHD
 Traumatic brain injury
 Narcolepsy
 Chronic fatigue syndrome
 Brand names include
 Ritalin (Ritalina, Rilatine)
 Attenta, Concerta
 Metadate, Methylin, Rubifen
 Focalin (dextro-methylphenidate)
 Daytrana (transdermal patch)
Stimulants
Methamphetamine
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Also known as: Methyl amphetamine or desoxyephedrine
Rx for ADHD or narcolepsy under the brand name Desoxyn
Used illegally for recreational purposes
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It is prone to abuse and addiction
Rapidly enters the brain and triggers a cascading release of
norepinephrine, dopamine and serotonin
Users may become obsessed or perform repetitive tasks
such as cleaning, hand-washing, or assembling and
disassembling objects
Withdrawal is characterized by excessive sleeping, eating
and depression-like symptoms, often accompanied by
anxiety
Users often take benzodiazepines as a means of "coming
down"
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 “crystal meth" refers to the crystalline (smokeable
form)
Stimulants
Methcathinone
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Potent CNS stimulant
Controlled substance
No clinical use at present
Used as antidepressant during 1930-40
Snorted, smoked, injected, or ingested
Chronic abuse may result in acute mental
confusion ranging from mild paranoia to
psychosis
Stimulants
Cocaine
 Stimulant of CNS
 Appetite suppressant
 Produce euphoric feelings
 Increased energy
 Most often used recreationally
 Used in medicine as a topical
anesthetic:
 eye, nose and throat surgeries
History of Cocaine
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In 1879 cocaine was used to treat morphine addiction
In 1884 cocaine is introduced as a local anesthetic
In 1885 Parke-Davis sold cocaine in various forms,
including cigarettes, powder, and as a mixture that
could be injected
Park-Davis promised that cocaine products would:
“supply the place of food, make the coward brave, the silent
eloquent and render the sufferer insensitive to pain”
In 1886 Coca-Cola included cocaine in its formula
In 1903 cocaine is eliminated from Coca-Cola
In 1914 the Harrison Narcotics Tax Act outlawed use of
cocaine
This law incorrectly referred to cocaine as a narcotic
Cocaine is a stimulant, not a narcotic
Forms of cocaine
 Cocaine Sulfate
 Produced by macerating coca leaves with water that
has been acidulated with sulfuric acid, or a solvent,
like kerosene or benzene.
 Often accomplished by putting the ingredients into a
vat and stamping on it, similar to the method for
crushing grapes in wine production.
 When water is evaporated will yield a pasty mass
 Cocaine Sulfate is intermediate step to producing
cocaine hydrochloride (salt form)
 It is commonly sold in South America as a pasty
mass
 Also known as pasta, basuco, basa, pitillo, paco
 Smoked along with tobacco
Freebase Cocaine
 Base form of cocaine
 Cocaine base is insoluble in water and is therefore not
suitable for drinking, snorting or injecting
 Smoking freebase is preferred by many because
cocaine is absorbed immediately into blood via the
lungs, reaching the brain in about five seconds
 Rush is more intense than sniffing the same amount
of cocaine nasally
 Peak of rush is over almost as soon as the user
exhales
 High typically lasts 5–10 minutes afterward
Crack Cocaine
Another form, of freebase
Often called "crack" or "rocks“
Created during early 1980s
Popular because it is cheap
Sodium bicarbonate (baking soda) is
preferred in preparing the freebase
 Commonly "cooked" the ratio of 50/50 to
40/60 % cocaine/bicarbonate
 When the rock is heated, the water boils,
making a crackling sound
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Chewed/eaten
 Coca leaves typically are mixed with an
alkaline substance (such as lime) and
chewed in the same way as chewing
tobacco
 It is absorbed by the mucous membrane of
the mouth and GI tract
 Coca leaves can be infused in liquid and
consumed like tea
 Not readily absorbed when ingested alone
 Need to be mixed with a highly alkaline
substance (such as lime) to be absorbed
through the stomach
Coca Leaf Infusions
Coca Tea
 Coca tea is used in coca-leaf producing countries
much as any herbal medicinal tea.
 The free and legal commercialization of dried coca
leaves to be used as "coca tea" has been actively
promoted by the governments of Peru and Bolivia for
many years as a drink having medicinal powers.
 Visitors to the city of Cuzco in Peru, and La Paz in
Bolivia are greeted with the offering of coca leaf
infusions (prepared in tea pots with whole coca
leaves) purportedly to help the newly-arrived
 The effects of drinking coca tea are a mild stimulation
and mood lift
 It does not produce any significant numbing of the
mouth nor does it give a rush like snorting cocaine
Insufflation
“snorting," “sniffing," or "blowing"
 Powder cocaine
 The most common method of ingestion
 Drug is absorbed through mucous membrane of
sinuses
 Absorption is approximately 30-60 %
 Chronic use results in rhinitis and necrosis of the
nasal membranes
 Damage the inside of the nose since cocaine
constricts blood vessel
 Users report a burning sensation in the nostrils after
cocaine's anesthetic effects wear off
 Rolled up banknotes, hollowed-out pens, cut straws,
and specialized spoons are often used to insufflate
cocaine
Injected Cocaine
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The highest blood levels of drug in the shortest amount of time
Upon injection, cocaine reaches the brain in a matter of
seconds
 rush can be so intense that can induces uncontrollable
vomit
Euphoria passes quickly
Aside from the toxic effects of cocaine, there is danger of
 circulatory emboli from the substances used to cut the drug
 risk of infection associated with use of contaminated
needles
Speedball
 Injected mixture of cocaine and heroin
 Dangerous combination, as drugs complement each other
Stimulants
Ecstasy/MDMA
 Methylenedioxymethamphetamine
 Often known as E, X, or XTC
 Primary effect is inducing a general sense of
openness, energy, euphoria, and well-being
 Tactile sensations are enhanced, making
physical contact with others more pleasurable
 May produce aphrodisiac effects
 A patent for MDMA was granted in 1914 to the
German pharmaceutical company Merck
 It was patented as an intermediate chemical
used in the synthesis of a hydrastinine (a drug
intended to control bleeding from wounds)
Hallucinogens
 Can cause subjective changes in
perception, thought, emotion and
consciousness
 Induce experiences that are qualitatively
different from those of ordinary
consciousness
 Three broad categories
 Psychedelics
 Dissociatives
 Deliriants
Hallucinogenous
 Cannabis sativa
 Herbal form of the drug consists of
dried mature leaves of pistillate
("female") plants
 Hashish (resinous form)
 Carefully produced and screened
hashish is up to three times as potent
as the highest quality herbal varieties
 Active chemical compound in cannabis
is: Δ9-tetrahydrocannabinol (THC)
Psychedelic
Any drug with perception-altering effects such as
 Lysergic acid diethylamide (LSD), semisynthetic drug
 synthesized from lysergic acid derived from ergot,
a grain fungus that grows on rye
 Psilocybin (psilocybine)
 found in psilocybin mushroom
 Mescaline occurs naturally in the
 Peyote cactus, San Pedro cactus, Peruvian Torch
cactus
 Ayahuasca preparations (use for religious purposes)
 Seeds of Morning Glory & Hawaiian Baby Woodrose
Dissociatives Drugs
 Reduce (or block) signals to the conscious mind from
other parts of the brain, typically the physical senses
 Such a state of sensory deprivation can produce
hallucinations, and dreamlike states of mind
 Some are
 PCP (angel dust)
 Ketamine (an anaesthetic)
 DXM (dextromethorphan) active ingredient in many
cough syrups
 nitrous oxide (inhalant)
 salvia divinorum (plant)
Deliriants
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Deliriants - effects similar to experience of delirious fevers
Considered to be true hallucinogens as users will
 have conversations with people who aren't there
 become angry with a 'person' mimicking their actions, not
realizing it is their own reflection in a mirror
Included in this group are:
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 deadly nightshade, mandrake, henbane and datura
Pharmaceutical drugs when taken in very high doses:
 antihistamine diphenhydramine (Benadryl)
 antiemetic dimenhydrinate (Dramamine or Gravol)
 Native Americans can consumed large amounts of tobacco
during religious ceremonies to experience deliriant effects.
Can be toxic, can cause death due to overdose.
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Plants such a:
Metabolisms and Elimination
 Elimination of most drugs by
 enzymes synthesized by liver
 Some are deactivates by being
passed in:
 urine, sweat, feces, mother's milk
Drug Tolerance
 Decreased sensitivity to a drug
 Same doses has less effect
 Need more drug to have same effect
 Cross tolerance
 Tolerance to the effect of one drug that develops
as the result of exposure to another drug that act
by same mechanism
Drug Tolerance
Two type of changes
 Metabolic Tolerance
 results from a reduction in the amount of
a drug getting to its sites of action
 Functional Tolerance
 results from a reduction in the reactivity
of the nervous system (or other sites of
action) to a drug
 Tolerance to psychoactive drugs mainly
fuctional