ANALGESICS

By: Sathish Rajamani

INTRODUCTION
Analgesics are medications used to relieve pain without reducing the consciousness of the patient. They work by reducing the amount of pain felt and this is generally achieved by interfering with the way the pain message is transmitted by the nerves. Analgesics will not treat the cause of the pain but they will provide temporary relief from pain symptoms.

TYPES OF ANALGESICS

OPIOID ANALGESICS
The opioid analgesics which are prescription only medicines that are very potent, being chemically related to morphine. Opioid analgesics are prescribed for moderate to severe pain, particularly of visceral origin, and are used in step two and step three of the analgesic ladder.

Dependence and tolerance are well known features with regular use although this should not inhibit prescribing in palliative care. Some chronic non-malignant conditions benefit from analgesic control with opioids, but patients should be reviewed regularly.

OPIUM, the greek name for poppy juice. Is obtained from the juice of the papaver somniferum.

ACTIONS OF OPIOID ANALGESICS

Opioid analgesics interacts with four major receptors in the CNS

Mu receptors Kappa receptors Sigma receptors and Delta receptors

RECEPTORS

EFFECTS
Analgesia, Respiratory depression and euphoria

MU

KAPPA

Respiratory depression, sedation Hallucination, Dysphoria, Seizures Analgesia

SEGMA
DELTA

CLASSIFICATION OF OPIOID ANALGESICS

Natural Alkaloids Morphine Codeine Semi Synthetic Compounds Pethidine Methadone Tramadol

MORPHINE
Morphine is the most important alkaloid of of opium. Morphine produces analgesia through actions in the brain and spinal cord. Morphine is readily absorbed from the GI tract and subcutaneous and muscle tissue. Morphine is administered intravenously, epidurally, and intrathecally.

PHARMACOTHERAPEUTICS
Morphine sulfate is primarily used to relieve moderate to severe pain. It is used pre operatively, its effect is on reducing patients anxiety and in assisting in induction of anesthesia. It is the drug of choice for clients with pain from MI, Pulmonary edema and dyspnea from acute left ventricular failure.

PHARMACOKINETICS

Absorption It depends on the route of administration, Morphine ingested orally is generally absorbed in one and half to two hours. It reaches liver for metabolism before reaching systemic circulation. Absorption after IM or SC injection occurs in 30 to 60 minutes.

PHARMACOKINETICS

Distribution It occurs quickly., After administration morphine leaves the blood and directly enters the kidney, lungs, liver and spleen. Its action on skeletal muscle is limited, since the drug is not very lipid soluble, it does not cross the BBB easily .

DURATION OF ACTION
METHOD OF ADMINISTRATION ONSET OF ACTION

Oral

4 to 12 hours

IM or SC

10 to 30 minutes

IV

15 to 30 minutes

PHARMACOKINETICS
BIOTRANSFORMATION

It occurs in the liver. Excretion occurs in the kidney. Only traces of morphine is founded in body after 48 hours. .

PHARMACODYNAMICS
Morphine produces analgesia by binding preferentially to the mu and delta receptors. Morphine targets the areas involved with regulation of pain perception, respiration and affective behaviors.

THERAPEUTIC USES
Analgesia Suppression of cough and dyspnea. Sedation In the treatment of diarrhea As preanesthetic medication In the treatment of the left ventricular failure.

CONTRAINDICATIONS
Head Injury, because morphine can cause increased intracranial tension, which can leads to marked respirator depression. Myxedema Bronchial asthma Morphine releases histamine which can trigger bronchoconstriction. Elderly patients In hypotensive states.

ADVERSE REACTIONS
CNS Side effects Confusion, anxiety, lethargy, nausea and vomiting. GIT Side effects Constipation Other Side effects Urinary retention, dry mouth, dysphoria, hypotension, skin rash, itching and urticaria.

MORPHINE POISONING
Acute poisoning with morphine and other opioids occurs with overdoses. Signs and Symptoms Coma, Pinpoint pupils, and respiratory depression which frequently called triad. TREATMENT Administration of antagonist Naloxone. Support of Respiratory and Cardio Vascular function.