1.

Introduction
Pethidine is an analgesics drug which is the synthesized form Morphine. For the better
understanding of Pethidine some term or concepts have to be defined. First of all opiates-it
is a term which signifies several drugs that are derived directly from opium, such as
morphine and codeine. An opioid, however, is a broader term for all substances that are used
as opiate. Now analgesics denote the drugs which relive pain. Though pethidine is
synthesized as a painkiller for medical use but it is not our concern. In this report we try to
show the negative use of pethidine as drug, its use, history, technique of use, effects,
mechanism of work etc.
2. Objectives
The report is conducted by following some objectives. The objectives are To know the historical background of pethidine;
To know what is pethidine;
Source of Pethidine;
Nature or State of Pethidine;
The way of pathedine consumption;
Pharmacokinetics ;
Mechanism of pethidine in body;
Uses of Pethidine ;
Effects: Adverse effects;
Interactions;
Dependence and Withdrawal Effects.

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3. Discussion
3.1 Definition of pethidine
Pethidine commonly referred to as Demerol is a fast-acting opioid analgesic drug. It's an
opiate drug (derived from the opium or poppy plant) so it's rather similar to morphine - in
fact, it is a synthetic version of morphine.
3.2 History of pethidine

The use of opiates can be traced back to at least 4000 BC where the products of
the opium poppy, Papaver somniferum, were taken by Sumerians, and to 2000
BC, when these drugs were used by the Egyptians.

Pethedine is synthesized from morphine in 1939 as a potential anticholinergic

agent by the German chemist Otto Eisleb.

its analgesic properties were first recognized by Otto Schaumann while working
for IG Farben, Germany.

For much of the 20th century, pethidine was the opioid of choice for many
physicians; in 1975, 60% of doctors prescribed it for acute pain and 22% for
chronic severe pain.

3.3 Sources of pethidine

Natural Opium Alkaloids

Poppy Tree

Morphine and Codeine

Semi-synthetic
Heroin

Synthetic
Pethidine
Fig 1: Sources of Pethidine
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Poppy tree is the primary sources of pethidine

Morphine is the secondary sources of Pethidine.

It is a synthetic version of Morohine.

3.4 Nature or State of pethidine

Pethidine can be found in three form.
1. Syrup
2. Tablets
3. Solution

3.5 How is Pethidine taken?

The three form of Pathedine is taken by orally and injections.
1. By mouth (orally) as tablets or syrup
2. Injection (Intramuscular or Intravenous)

3.6 Pharmacokinetics of Pethidine

Well absorbed orally, bioavailability 50%
Effects appear in 10-15 min. after oral absorption
On parenteral administration action lasts for 2-3 Hrs
Metabolized in liver mepiridinic acid and norpethidine
Norpethidine accumulates on chronic use
Excreted in urine
Dosage is based on your age, gender, medical condition, response to therapy, and use
of certain interacting medicines.

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3.7 Mechanism of Pethidine in Body

Opioid drugs, typified by morphine, Pethidine produce their pharmacological actions,
including analgesia, by acting on receptors located on neuronal cell membranes. The
presynaptic action of opioids to inhibit neurotransmitter release is considered to be their
major effect in the nervous system.

Recent advances in the molecular biology of opioid receptors has confirmed that
there are 3 types of opioid receptor, m, d and k.

All are coupled to intracellular mechanisms via G-proteins.

Opioids receptors
Opioids produce effects on neurons by acting on receptors located on neuronal cell
membranes. Three major types of opioid receptor, m, d and k (mu, delta and kappa).

Fig 2: Human m opioid receptor

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Fig 3: action of G-protein.

Like morphine, pethidine exerts its analgesic effects by acting as an agonist at the opioid receptor

Pethidine is often employed in the treatment of postanesthetic shivering. The

pharmacologic mechanism of this antishivering effect is not fully understood,[19] but it
may involve the stimulation of -opioid receptors.

3.8 Uses of Pethidine

Pethidine is a painkiller
It is used as an analgesic for the relief of moderate to severe pain
Pain relief during childbirth.

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 Pain relief before, during and after an operation.

3.9 Effects of Pethidine
Adverse effects

The adverse effects of pethidine

administration are primarily those
of the opioids as a class:

nausea, vomiting,

sedation,

dizziness, or spinning sensation

Diaphoresis

Pinpoint pupils (miosis).

Problems with urinating: urinary

constipation

Feeling weak.

Increased blood flow to the skin on

the face.

Feeling of well-being (euphoria) or

changes in mood.

False perceptions of things that are

not really there.

(respiratory depression).

retention

Drowsiness

Dry mouth.

Headache.

Confusion

Rash or itching

Slow, shallow breathing

Awareness of your heartbeat.

Increased or decreased heart rate

(tachycardia).

Low blood pressure (hypotension).

Feeling cold.

3.10 Interaction with other drugs

The sedative effect of this medicine will be increased if this medicine is taken with any of the
following, which can also cause drowsiness:

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Alcohol

Antipsychotics, e.g. chlorpromazine

Barbiturates, e.g. amobarbital

Benzodiazepines, e.g. diazepam

Certain antiepileptic's, such as sodium valproate

Other strong opioid painkillers, e.g. morphine, codeine

Sedating antihistamines, e.g. hydroxyzine

Sleeping tablets, e.g. zopiclone

Tricyclic antidepressants, e.g. amitriptyline

3.11 Dependence and Withdrawal Effects

As for Opioid Analgesics, Doses of pethidine as large as 3 or 4 g daily have been taken by
addicts. As tolerance to the CNS stimulant and anti-muscarinic effects is not complete with
these

Withdrawal symptoms appear more rapidly than with morphine and are of shorter
duration.

Early symptoms typically begin in the first 24 hours after you stop using the drug, and
they include:
muscle aches
restlessness
anxiety
lacrimation (eyes tearing up)
runny nose
excessive sweating
inability to sleep
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 yawning very often

Later symptoms, which can be more intense, begin after the first day or so. They
include:
diarrhea
abdominal cramping
goose bumps on the skin
dilated pupils and possibly blurry vision
rapid heartbeat
high blood pressure

4.

Conclusion

Pethidine is a potent analgesic which produces a prompt but short-lasting analgesia - the half
life is around two hours. Thus, it is not useful in the management of terminal care, but may
be used in situations such as childbirth, especially as it has been suggested that it has less
effect on the respiratory rate than the opiate analgesics. Even in this case, it may be necessary
to administer narcotic antagonists. It has been used for peri-operative analgesia but in many
ways it has been surpassed by newer drugs with lesser side effects.

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5. References
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Jaffe, J. H. Opioid-related disorders. In B. J. Sadock & V. A. Sadock (Eds.),Comprehensive
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