PHARMACOLOGICAL

PROPERTIES
CLEMENTINO I
AMPHETAMINE (STIMULANT)
• Amphetamine [am-FET-a-meen] is a sympathetic amine that shows
neurologic and clinical effects quite similar to those of cocaine.
• INDICATION: Attention deficit hyperactivity disorder (ADHD),
Narcolepsy, Appetite suppression
• Contraindications: Patients with hypertension, cardiovascular disease,
hyperthyroidism, glaucoma, or a history of drug abuse or those taking
MAO inhibitors
• Pharmacokinetic: completely absorbed from the GI tract,
metabolized by the liver, and excreted in the urine.
• Amphetamine abusers often administer the drugs by IV injection
and/or by smoking. The euphoria caused by amphetamine lasts 4 to 6
hours, or four- to eightfold longer than the effects of cocaine.
• MOA:
• ADR:The amphetamines may cause addiction, leading to dependence,
tolerance, and drug-seeking behavior. In addition, they have the
following undesirable effects.
BENZODIAZEPINES
• EFFECTS: SEDATIVE-HYPNOTIC
COCCAINE (STIMULANT)
• Cocaine is derived from the erythroxylon coca shrub that grows in the
foothills of the Andes Mountains in South America.
• For more than 100 years, it has been extracted and used in clinical
medicine, mainly as a local anesthetic and to dilate pupils in
ophthalmology.
• Sigmund Freud famously proposed its use to treat depression and
alcohol dependence, but addiction quickly brought an end to this
idea.
• Cocaine hydrochloride is a water-soluble salt that can be injected or
absorbed by any mucosal membrane.
• When heated in an alkaline solution, it is transformed into the free
base, “crack cocaine,” which can then be smoked.
• Inhaled crack cocaine is rapidly absorbed in the lungs and penetrates
swiftly into the brain, producing an almost instantaneous “rush.”
• The primary mechanism of action underlying the effects of cocaine is
blockade of reuptake of the monoamines (norepinephrine, serotonin,
and dopamine) into the presynaptic terminals.
• This potentiates and prolongs the CNS and peripheral actions of these
monoamines.
• In particular, the prolongation of dopaminergic effects in the brain’s
pleasure system (limbic system) produces the intense euphoria that
cocaine initially causes.
MARIJUANA (HALLUCINOGEN)
• Cannabis is a plant that is thought to have been used by humans for
over 10,000 years.
• Today, marijuana is the most frequently used illicit drug, and the illicit
drug that new users are most likely to try
• the species Cannabis sativa is the plant most often used for its
hallucinogenic properties.
• The main psychoactive alkaloid contained in marijuana is Δ9-
tetrahydrocannabinol (THC).
• EFFECT: physical relaxation, hyperphagia (increased appetite),
increased heart rate, decreased muscle coordination, conjunctivitis,
and minor pain control, euphoria, followed by drowsiness and
relaxation
• MOA: Specific receptors in the brain, cannabinoid or CB1 receptors,
were discovered in the late 1980s and found to be reactive to THC.
• Pharmacokinetic: The effects of THC appear immediately after the
drug is smoked, but maximum effects take about 20 minutes. By 3
hours, the effects largely disappear.
• Marijuana stimulates the amygdala, causing the user to have a sense
of novelty to anything the user encounters through an enhancement
of sensory activity.
• The effects of marijuana on γ-aminobutyric acid (GABA) in the
hippocampus diminish the capacity for short-term memory in users,
and this affect seems to be more pronounced in adolescents.
• Long-term effects of use may include chronic bronchitis, chronic
obstructive pulmonary disease, increased progression of HIV and
breast cancer, and exacerbation of mental illness.
• Withdrawal may include depression, pain, and irritability.
HEROIN (OPIOID)
•  Heroin can be traced back to some structural properties of the
morphine molecule.
• The analgesic effects of heroin derive from the two active
metabolites, 6-O-acetylmorphine and morphine, which bind
specifically to the mu-opioid receptors of the central nervous system.
• Pharmacokinetic: significant first-pass metabolism of heroin occurs in the
liver, intramuscular, subcutaneous, and IV injections produce the most reliable
responses. Heroin rapidly enters all body tissues, including the fetuses of
pregnant women.
• Heroin is more potent and faster acting than morphine as an analgesic drug.
• Tolerance to opioids is due to increased adaptation of the cells which changes
their receptor sites after chronic exposure to the drug.
• Withdrawal pro- duces a series of autonomic, motor, and psychological
responses that incapacitate the individual
• ADR: severe respiratory depression can occur and may result in death from
acute opioid overdose.