Potent Opiate Analgesic Medication Biology Essay

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Morphine is a potent opiate analgesic medication and is considered to be the prototypical opioid. It was discovered in 1804 by Friedrich Sertrner, first distributed by same in 1817, and first commercially sold by Merck in 1827, which at the time was a single small chemists shop. It was more widely used after the invention of the hypodermic needle in 1857. It took its name from the Greek God of dreams Morpheus .

Morphine is the most abundant alkaloid found in opium, the dried sap (latex) derived from shallowly slicing the unripe seedpods of the opium, or common or edible, poppy, Papaver somniferum. Morphine was the first active principle purified from a plant source and is one of at least 50 alkaloids of several different types present in opium, Poppy Straw Concentrate, and other poppy derivatives.

. The human body also produces small amounts of morphine and metabolises it into a number of other active opiates.

In clinical medicine, morphine is regarded as the gold standard, or benchmark, of analgesics used to relieve severe or agonizing pain and suffering.

morphine acts directly on the central nervous system (CNS) to relieve pain. Morphine has a high potential for addiction; tolerance and psychological dependence develop rapidly, although physical addiction may take several months to develop.


An opium-based elixir has been ascribed to alchemists of Byzantine times, but the specific formula was supposedly lost during the Ottoman conquest of Constantinople

Around 1522, Paracelsus made reference to an opium-based elixir that he called laudanum

He described it as a potent painkiller, but recommended that it be used sparingly. In the late eighteenth century, when the East India Company gained a direct interest in the opium trade through India, another opiate recipe called laudanum became very popular among physicians and their patients.

Morphine was discovered as the first active alkaloid extracted from the opium poppy plant in December 1804 in Paderborn, Germany, by Friedrich Sert'rner

The drug was first marketed to the general public by Sert'rner and Company in 1817 as an analgesic, and also as a treatment for opium and alcohol addiction. Commercial production began in Darmstadt, Germany in 1827 by the pharmacy that became the pharmaceutical compary Merck, with morphine sales being a large part of their early growth.[

Later it was found that morphine was more addictive than either alcohol or opium, and its extensive use during the American Civil War allegedly resulted in over 400,000[4] sufferers from the "soldier's disease" of morphine addiction

Diacetylmorphine (better known as heroin) was synthesized from morphine in 1874 and brought to market by Bayer in 1898. Heroin is approximately 1.5 to 2 times more potent than morphine on a milligram-for-milligram basis. Due to the lipid solubility of diacetylmorphine, it is able to cross the blood-brain barrier faster than morphine, subsequently increasing the reinforcing component of addiction.

Morphine became a controlled substance in the US under the Harrison Narcotics Tax Act of 1914, and possession without a prescription in the US is a criminal offense

The structural formula of morphine was determined by 1925. At least three methods of total synthesis of morphine from starting materials such as coal tar and petroleum distillates have been patented, the first of which was announced in 1952, by Dr. Marshall D. Gates, Jr. at the University of Rochester

In 2003, there was discovery of endogenous morphine occurring naturally in the human body. Thirty

Human cells that form in reaction to cancerous neuroblastoma cells have been found to contain trace amounts of endogenous morphine.[14]

[edit] Indications

Morphine can be used as an analgesic to relieve:

pain in myocardial infarction

pain in sickle cell crisis

pain associated with surgical conditions, pre- and postoperatively

pain associated with trauma

severe chronic pain, e.g., cancer[15]

pain from kidney stones (renal colic, ureterolithiasis)

severe back pain

Morphine can also be used:

as an adjunct to general anesthesia

in epidural anesthesia or intrathecal analgesia

for palliative care (i.e., to alleviate pain without curing the underlying reason for it, usually because the latter is found impossible)

as an antitussive for severe cough

in nebulized form, for treatment of dyspnea, although the evidence for efficacy is slim.[16] Evidence is better for other routes.[17]

as an antidiarrheal in chronic conditions (e.g., for diarrhea associated with AIDS, although loperamide (a non-absorbed opioid acting only on the gut) is the most commonly used opioid for diarrhea).

for relief of acute pulmonary edema through an unknown mechanism

for lowering and stabilising blood glucose in diabetics and combating other diabetic effects including diabetic neuropathy

Morphine will also impact hypertension, chronic pain patients today, some doctors prescribe morphine and other opiates off label for depression, anxiety, and other mental illness.

Side effects

[edit] Constipation

Like loperamide and other opioids, morphine acts on the myenteric plexus in the intestinal tract, reducing gut motility, causing constipation


By inhibiting gastric emptying and reducing propulsive peristalsis of the intestine, morphine decreases the rate of intestinal transit

Equipotent, injected doses had comparable action courses, with no difference in subjects' self-rated feelings of euphoria, ambition, nervousness, relaxation, drowsiness, or sleepiness.[10] Short-term addiction studies by the same researchers demonstrated that tolerance developed at a similar rate to both heroin and morphine

former addicts showed a strong preference for heroin and morphine, suggesting that heroin and morphine are particularly susceptible to abuse and addiction

and most studies on morphine addiction merely show that "severely distressed animals, like severely distressed people, will relieve their distress pharmacologically if they can

Morphine is a potentially highly addictive substance. It can cause psychological dependence and physical dependence as well as tolerance, with an addiction potential identical to that of heroin. When used illicitly, a very serious narcotic habit can develop in a matter of weeks,


Tolerance to the analgesic effects of morphine is fairly rapid

CCK-antagonist drugs, specifically proglumide, have been shown to slow the development of tolerance to morphine.

[edit] Withdrawal

Cessation of dosing with morphine creates the prototypical opioid withdrawal syndrome, which

is not fatal by itself in neurologically healthy patients without heart or lung problems; it is in theory self-limiting in length and overall impact in that a rapid increase in metabolism and other bodily processes takes place, including shedding and replacement of the cells of many organs

Nonetheless, suicide, heart attacks, strokes, seizures proceeding to status epilepticus, and effects of extreme dehydration do lead to fatal outcomes in a small fraction of cases.

The withdrawal symptoms associated with morphine addiction are usually experienced shortly before the time of the next scheduled dose, sometimes within as early as a few hours (usually between 6'12 hours) after the last administration. Early symptoms include watery eyes, insomnia, diarrhea, runny nose, yawning, dysphoria, sweating and in some cases a strong drug craving. Severe headache, restlessness, irritability, loss of appetite, body aches, severe abdominal pain, nausea and vomiting, tremors, and even stronger and more intense drug craving appear as the syndrome progresses. Severe depression and vomiting are very common.

Chills or cold flashes with goose bumps ("cold turkey") alternating with flushing (hot flashes), kicking movements of the legs ("kicking the habit"[25]) and excessive sweating are also characteristic symptoms.

Long after the physical need for morphine has passed, the addict will usually continue to think and talk about the use of morphine (or other drugs) and feel strange or overwhelmed coping with daily activities without being under the influence of morphine. Psychological withdrawal from morphine is a very long and painful process

Abusers of morphine (and heroin) have one of the highest relapse rates among all drug users, ranging up to 98 per cent in the estimation of some clinicians, neuropharmacologists, mental health/AODA professionals and other medical experts

] Overdose

A large overdose can cause asphyxia and death by respiratory depression if the person does not receive medical attention immediately.[31] Treatments include administration of activated charcoal, intravenous fluids, laxatives and naloxone. The latter completely reverses morphine's effects, but precipitates immediate onset of withdrawal in opiate-addicted subjects. Multiple doses may be needed

The minimum lethal dose is 200 mg but in case of hypersensitivity 60 mg can bring sudden death. In case of drug addiction, 2-3 g/day can be tolerated

] Contraindications

contraindications for morphine:

acute respiratory depression

renal failure

raised intracranial pressure, including head injury

chemical toxicity

Gene expression

Studies have shown that morphine can alter the expression of a number of genes. A single injection of morphine has been shown to alter the expression of two major groups of genes, for proteins involved in mitochondrial respiration and for cytoskeleton-related proteins

] Effects on the immune system

Morphine has long been known to act on receptors expressed on cells of the central nervous system resulting in pain relief and analgesia. In the 1970s and '80s, evidence suggesting that opiate drug addicts show increased risk of infection (such as increased pneumonia, tuberculosis, and HIV) led scientists to believe that morphine may also affect the immune system. This possibility increased interest in the effect of chronic morphine use on the immune system.

morphine influences the production of neutrophils and other cytokines. Since cytokines are produced as part of the immediate immunological response (inflammation), it has been suggested that they may also influence pain.

Effects on human performance

that morphine may have a negative impact on anterograde and retrograde memory,[47] but these effects are minimal and are transient

Morphine has resulted in impaired functioning on critical flicker frequency (a measure of overall CNS arousal) and impaired performance on the Maddox Wing test (a measure of deviation of the visual axes of the eyes).

A Hungarian chemist, J'nos K'b'y, developed in 1925 and internationally patented in 1930 a method to extract morphine from dried poppy straw.

Morphine is known on the street and elsewhere as M, Number

glad stuff, happy stuff, happy powder, white nurse, Red Cross, first line, unkie, mojo, God's Own Medicine, Vitamin M, Emma. Emmy, Lady M, white lady, cube, cube juice, mo, morf, morph, morpho, Miss Emma, mofo, hard stuff

big M

Morphine can be smoked,injected.

2681351 morphine book.html:

Pharmacology: Morphine is the principal alkaloid of opium and is a potent analgesic and sedative agent. After intravenous injection, peak analgesia is attained within 20 minutes and usually lasts 3'5 hours.


A. Known hypersensitivity to morphine.

B. Respiratory or CNS depression with impending respiratory failure unless the patient is already intubated or equipment and trained personnel are standing by for intervention if necessary with intubation or the reversal agent naloxone (see Naloxone and Nalmefene).

C. Suspected head injury. Morphine may obscure or cause exaggerated CNS depression.

Adverse effects:

A. Respiratory and CNS depression may result in respiratory arrest. Depressant effects may be prolonged in patients with liver disease and chronic renal failure

lacking tolerance, hypothyroidism, morbid obesity, and sleep apnea syndrome

Dosage and method of administration:

A. Morphine may be injected subcutaneously, intramuscularly, or intravenously. The oral and rectal routes produce erratic absorption and are not recommended for use in acutely ill patients.

B. Hypotension may occur owing to decreased systemic vascular resistance and venous tone.

C. Nausea, vomiting, and constipation may occur.

D. Bradycardia, wheezing, flushing, pruritus, urticaria, and other histamine-like effects may occur.

E. Sulfite preservative in some parenteral preparations may cause hypersensitivity reactions.

F. Use in pregnancy. FDA category C (indeterminate). This does not preclude its acute, short-term use in a seriously symptomatic patient.

history of medicine\poster\Morphine Medicine Patient UK.mht

' Morphine can also cause drowsiness.

' Morphine is used to treat severe pain or severe coughing.

' Nausea, vomiting or constipation may occur with this medicine.

' Morphine is used to relieve severe pain and severe coughs; it works on the nerves and brain to reduce the pain you feel or the need to cough.

Before taking morphine make sure your doctor or pharmacist knows:

' If you are pregnant, trying for a baby or breast-feeding.

' If you have liver, kidney or prostate problems.

' If you have heart rhythm problems.

' If you have breathing problems, such as asthma.

' If you have low blood pressure.

' If you have thyroid problems.

Side effects: Constipation Dry mouth, Dizziness, particularly when getting up from a sitting or lying position, Other side-effects include: palpitations, swollen legs or ankles, mood changes, confusion, sleep disturbances, headache, sexual difficulties, difficulty passing urine, sweating, rash, and itching.

Morphine Information from Drugs_com.mht

Morphine is in a group of drugs called narcotic pain relievers.

Morphine is used to treat moderate to severe pain. It works by dulling the pain perception center in the brain. Short-acting formulations are taken as needed for pain. Extended-release formulations are used when around-the-clock pain relief is needed.

Morphine is not for treating pain just after surgery unless you were already taking it before the surgery.

Morphine may also be used for purposes other than those listed in this medication guide.

Morphine side effects

Get emergency medical help if you have any of these signs of an allergic reaction to morphine: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have any of these serious side effects:

' shallow breathing, slow heartbeat;

' seizure (convulsions);

' cold, clammy skin;

' confusion;

' severe weakness or dizziness; or

' feeling light-headed, fainting.

Less serious morphine side effects are more likely to occur, such as:

' constipation;

' warmth, tingling, or redness under your skin;

' nausea, vomiting, stomach pain, diarrhea, loss of appetite;

' dizziness, headache, anxiety;

' memory problems; or

' sleep problems (insomnia).

' Morphine Summary BookRags_com.mht

' Morphine

' Morphine is the most effective naturally occurring compound used for the relief of pain in medicine and surgery. It also induces sleep and produces euphoria. The active ingredient in opium, from which it is derived, morphine is highly addictive with repeated use. Its story is the story of the founding of alkaloid chemistry, which grew out of the study of plant bases and plays an essential role in medicine. In 1805, opium was widely used for its euphoric effects, and a German pharmacist named Friedrich Sert'rner (1783-1841) decided to investigate the components of poppy juice, from which opium is derived. He found an unknown acid, converted it into a crystalline precipitate, and named it principium somniferum. Having determined that this substance was the active ingredient in opium, in 1809 he recommended the cultivation of the poppy on a large scale as a way to further the national economy since morphine was used in the production of the popular drug and poppy seed oil. In 1815, Sert'rner and three young volunteers each took three 30 mg doses of principium somniferum over a period of 45 minutes, and were not fully themselves again until several days later. In 1817, he published a paper describing the drug, in which he changed its name to morphium, after Morpheus, the Greek god of dreams. The same year, the name was changed to morphine by the French chemist Joseph Gay-Lussac.

' During the 1800s, the French physiologist Fran'ois Magendie advanced the use of morphine in medicine, administering it both orally and by injection. Morphine's greatest medical advantage is its depressant action that causes the threshold of pain to rise, relieving pain many other analgesics are unable to control.

' Morphine's popularity on the Civil War battlefields boosted its general use in the treatment of many kinds of discomfort, and a leading British doctor called morphine "God's own medicine."

' Once addicted, a person is likely to experience severe symptoms of withdrawal, including pain, hyperventilation, restlessness, and confusion. In 1898, the Bayer corporation synthesized heroin from morphine and marketed it as an antidote to morphine addiction, but the concurrent moral reform movements were beginning to give rise to anti-opiate sentiments, and morphine's popularity and acceptance began to decline. Today, morphine is used most often for short-term, post-operative pain control, while methadone is used to treat opiate addiction and for long-term pain control.



Morphine, C17H19NO3, is the most abundant of opium's 24 alkaloids

Named after the Roman god of dreams, Morpheus, who also became the god of slumber, the drug morphine, appropriately enough, numbs pain, alters mood and induces sleep


Morphine acts on a specific receptor of nerve cells. More specifically many such receptors are found in the spinal cord's substantia gelatinosa, a region where pain signals are first processed

Morphine Effects on HTLV-I Infection in the Presence or

Absence of Concurrent HIV-1 Infection



In the body, heroin is quickly converted to morphine

The two drugs exert similar effects on immunity by interacting with mu (m ) opioid receptors found on immune cells (Madden et al., 1998; Sharp et al., 1998). The immediate result of this opioid-receptor interaction is the suppression of certain facets of immune cell function, in particular

of transcription factors


In 1898 ' while trying to find a less addictive form of morphine ' the Bayer chemical cartel of Elberfeld, Germany, began manufacturing 'heroin' and launched a massive international marketing campaign. But heroin was far more addictive than morphine and was outlawed in 1923 by the US Government and the League of Nations.