Transcript Strong Analgesics

B 3.3 Strong Analgesics
Compare the structures
Morphine, codeine, heroine-semisynthetic
Advantages/disadvantages
Analgesics
Opium
Strong Analgesics
• Relief of very severe pain,
• include narcotics : heroin, codeine,
morphine
• Addictive
• Controlled substances
Strong
Analgesics
Morphine
• Morphine is used intravenously,
intramuscularly, subcutaneously, orally,
intra articular
Heroin
Strong Analgesics
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The Opium alkaloids
Narcotic / sleep inducing
analgesics /pain relieving
Morphine: alkaloid 10% by mass of raw
opium
• Codeine ~ 0.5 % by mass of raw opium
• Heroin : synthetic / acetylation of morphine
Meperidine
Administration
parenteral, oral
fentanyl
Demerol
DEMEROL has been reported as being abused by crushing, chewing,
snorting, or injecting the dissolved product. These practices will result
in the uncontrolled delivery of the opioid and pose a significant risk to
the abuser that could result in overdo
Methadone /dolophine
Blocks the euphoric high of heroin and is used in the
treatment of heroin addicts in some countries /as a legal
drug
Advantages
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Pharmacological effects on:
Central nervous system
The eye
Gastrointestinal tract
The prime medical uses of
opiates:
• Relief of severe pain caused by injury,
cancer, surgery (before/afterward
• Treatment of diarrhea by producing
constipating effect
• To relieve coughing by suppressing the
cough center
• Addictive nature of opiates/ it is replaced by
synthetic non-narcotic drug
Psychological effects of Opiates
• Analgesia, drowsiness, mood changes
and mental clouding
• Anxiety, fear, lethargy, sedation, lack of
concern, inability to concentrate, nausea
and vomiting
• Users feel a relief from emotional and
psychological pain
Tolerance and Dependence
• Due to the induction of drug metabolizing
enzymes in the liver
• And adaptation of neurons in the brain to
the presence of the drug
• Tolerance to all other opiates
Physical Dependence
• Need to take drug to function properly
• Withdrawal symptoms: restlessness,
sweating, fever, chills, vomiting, Increase
rate of respiration, unbearable aches /
pains
• Depends on dose
• Frequency of drug administration
• Duration of the drug dependence, the
opiate used
Opiates
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Extremely potent
Capacity to induce euphoria
Strong compulsion to misuse
Induce profound tolerance, physiological
dependence
• Lead to crime
Short term Effects
• Sedation, stupor; relief from pain
• Euphoria: impaired functioning and
coordination
• Reduced tension, worry, fear
• Reduced coughing reflux
• Occasional death from overdose
Long term effects
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Loss of appetite; malnutrition, constipation
Sterility
Withdrawal illness, loss of job, crime
Diversion of $ and energy
Risk of dangerous infections AIDS, due to
shared needles
Medical uses / Opiates
• Strong analgesics / pain reliever in cancer,
prior to and recovery from surgery
• Heroin / 3 times as morphine
• Codeine as 1/6th of morphine
• In the treatment of diarrhea by producing
constipation
• To relieve coughing by suppressing the
cough centers in brain
Local anesthetics
• Pain killers in localizes areas
• Lidocaine and procaine (Novocain)
• Used in dentistry
Novocain
• t is the first injectable local anesthetic to
be synthesized,
• commonly known as Novocain.
• The German Chemist, Alfred Einhorn,
developed it in 1904.
• Procaine is the precursor to cocaine.
• Procaine works to anesthetize a patient for
about 15 minutes. To prolong anesthesia
epinephrine is added as a vasoconstrictor.
Procaine/Cocaine
• Cocaine blocks Na+ passage
through the axon cell membrane
and
• inhibits the reuptake of Dopamine
and Serotonin
• resulting in psycho-stimulation.
Procaine
• Procaine blocks nerve conductance
via inhibiting Na+ at the membrane,
• thus no psycho-stimulation.
• Both reactions are brief.
• Drug Interactions?
• Procaine is thought to reduce the effects of
sulfonamide antibiotics.
• How is this medication administered?
• Oral injection.
Lidocaine
General Anesthetics B9-447
SEROTONIN,
happy neurotransmitter.
• 5-hydoxytryptamine, is naturally produced
in the pineal gland, which lies at the centre
of our brain.
• “It is essential to numerous body function
including appetite control, sleep, memory
and learning, temperature regulation,
mood, behavior, cardiovascular function,
muscle contraction, endocrine regulation
and depression.
DOPAMINE,
• 4-(2-aminoethyl)benzene-1,2-idol, is
produced in several areas of the brain
including the substantia nigra.
• It is central to movement coordination,
cognitive functions (by mediating signal
transduction in the frontal lobe thus
affecting memory, attention, and problemsolving in particular), latent inhibition and
creative drive.
Dopamine
• Its release is stimulated by naturally
rewarding experiences
• such as happy foods (bananas!), drugs,