Semester-IV

Sub Name-medicinal chemistry-I (sub code-BP-402T)

Objective
Sodium salicylate, Aspirin, Mefenamic acid*, Meclofenamate, Indomethacin, Sulindac,
Tolmetin, Zomepriac, Diclofenac, Ketorolac, Ibuprofen*, Naproxen, Piroxicam,
Phenacetin, Acetaminophen, Antipyrine, Phenylbutazone.

1. INTRODUCTION

A drug or substance that reduces inflammation (redness, swelling, and pain) in the body. Anti-
inflammatory agents block certain substances in the body that cause inflammation. They are used
to treat many different conditions. Some anti-inflammatory agents are being studied in the
prevention and treatment of cancer.

1.1 CLASSIFICATION

NSAIDs can be classified based on their chemical structure or mechanism of action. Older
NSAIDs were known long before their mechanism of action was elucidated and were for this
reason classified by chemical structure or origin. Newer substances are more often classified by
mechanism of action.
Salicylate

• Aspirin (acetylsalicylic acid)

• Diflunisal (Dolobid)
• Salicylic acid and its salts
Propionic acid derivatives

• Ibuprofen
• Dexibuprofen
• Naproxen
• Fenoprofen
• Ketoprofen
• Dexketoprofen
Acetic acid derivatives

• Indomethacin
• Tolmetin
• Sulindac
• Ketorolac
• Diclofenac
• Aceclofenac
• Nabumetone (drug itself is non-acidic but the active, principal metabolite has a carboxylic
acid group)

Enolic acid (oxicam) derivatives

• Piroxicam
• Meloxicam
• Tenoxicam
• Droxicam
• Lornoxicam
• Isoxicam (withdrawn from market 1985)
• Phenylbutazone
Anthranilic acid derivatives (fenamates)
The following NSAIDs are derived from fenamic acid. which is a derivative of anthranilic
acid, which in turn is a nitrogen isostere of salicylic acid, which is the active
metabolite of aspirin.

• Mefenamic acid
• Meclofenamic acid
• Flufenamic acid
• Tolfenamic acid
Selective COX-2 inhibitors (coxibs)

• Celecoxib
• Rofecoxib
• Parecoxib
• Etoricoxib
Sulfonanilides

• Nimesulide (systemic preparations are banned by several countries for the potential risk of
hepatotoxicity)

1.2 Mechanism of Action

NSAIDs are used for their analgesic, anti-inflammatory, and antipyretic properties. Their
therapeutic actions are thought to stem primarily from their ability to block the formation of
certain prostaglandins through inhibition of the cyclooxygenase (COX) enzymes (Figure 1). In
general, COX-1 catalyzes the production of several cytoprotective prostaglandins that coat the
stomach lining with mucus and aid platelet aggregation, among other functions. COX-2 catalyzes
the conversion of arachidonic acid into the inflammatory prostaglandins that are involved in
three key biological functions: sensitizing skin pain receptors, elevating body temperature
through the hypothalamus, and recruiting inflammatory cells toward injured body parts.

2.1 Aspirin
IUPAC NAME: 2-Acetoxybenzoic acid

Therapeupic uses:
• Aspirin is used in the treatment of a number of conditions, including fever,
pain, rheumatic fever, and inflammatory conditions, such as rheumatoid
arthritis, pericarditis, and Kawasaki disease.
• Lower doses of aspirin have also been shown to reduce the risk of death from a heart
attack, or the risk of stroke in people who are at high risk or who have cardiovascular
disease, but not in elderly people who are otherwise healthy.
• There is some evidence that aspirin is effective at preventing colorectal cancer, though
the mechanisms of this effect are unclear.
 Adverse Effects:-
• Aspirin should not be taken by people who are allergic to ibuprofen or naproxen, or who
have salicylate intolerance or a more generalized drug intolerance to NSAIDs, and
caution should be exercised in those with asthma or NSAID-precipitated bronchospasm.
• Owing to its effect on the stomach lining, manufacturers recommend people with peptic
ulcers, mild diabetes, or gastritis seek medical advice before using aspirin.

2.2 Sodium Salicylate:-

IUPAC NAME: Sodium o-hydroxybenzoate

Therapeutic Uses:-

• It is used in medicine as an analgesic and antipyretic. Sodium salicylate also acts as non-
steroidal anti-inflammatory drug (NSAID) and induces apoptosis in cancer cells and
also necrosis.
• It is also a potential replacement for aspirin for people sensitive to it.
• It may also be used as a phosphor for the detection of vacuum ultraviolet radiation and
electrons.
Adverse Effects:-
• Heartburn.
• Irritation of the Stomach or Intestines.
• Nausea.
• Stomach Cramps.
• Vomiting.
2.3 Mefenamic acid
IUPAC NAME: N-(2,3-Xylyl)-anthranilic acid
 Therapeutic Uses
• Mefenamic acid is used to treat moderate pain and menstrual pain.
• There is evidence that supports the use of mefenamic acid for perimenstrual migraine
headache prophylaxis, with treatment starting 2 days prior to the onset of flow or 1 day
prior to the expected onset of the headache and continuing for the duration
of menstruation.
Adverse Effects
• Headaches, nervousness, and vomiting.
• Serious side effects may include diarrhea, hematemesis (vomiting
blood), hematuria (blood in urine), blurred vision, skin rash, itching and swelling, sore
throat and fever.
• It has been associated with acute liver damage.

2.4 Meclofenamate
IUPAC NAME:2-[(2,6-dichloro-3-methyl phenyl)amino]benzoic acid

Therapeutic Uses

• Used for joint, muscular pain, arthritis and dysmenorrhea.

• It is a member of the anthranilic acid derivatives (or fenamate) class of NSAID drugs and
was approved by the FDA in 1980.
• Like other members of the class, it is a COX inhibitor and prevents formation
of prostaglandins.

Adverse Effects

• Nausea.
• Vomiting.
• Heartburn.
• Dizziness.
• Drowsiness.
• Diarrhea.

2.5 Indomethacin
IUPAC NAME: 1-(4-chlorobenzoyl) 5-methoxy-2-methylindol-3yl acetic acid

Therapeutic Uses

• rheumatoid arthritis
• ankylosing spondylitis
• osteoarthritis
• gouty arthritis

Adverse Effects

• Edema (swelling due to fluid retention)

• Hyperkalemia (high potassium levels)
• Hypernatremia (high sodium levels)
• Hypertension

2.6 Sulindac

IUPAC NAME: (Z)-5-Fluoro-2-methyl-1-[4-(methyl sulphinyl) benzylidene] indene-3yl acetic

acid

Therapeutic Uses
 • Like other NSAIDs, it is useful in the treatment
of acute or chronic inflammatory conditions.
• This is thought to help maintain constant blood levels with reduced gastrointestinal side
effects.

Adverse Effects
• nausea, vomiting, stomach pain, indigestion, loss of appetite;
• Diarrhea, constipation.
• Headache, dizziness, nervousness.
• Itching, rash.
• Ringing in your ears.

2.7 Tolmetin
IUPAC NAME: [1-methyl-5-(4-methyl benzoyl)-1H-Pyrrol-2-yl] acetic acid

Therapeutic uses
• Tolmetin is used alone or with other treatments to reduce pain, swelling, and joint
stiffness from rheumatoid arthritis and osteoarthritis.
• It is also used for juvenile rheumatoid arthritis.

Adverse Effects
• Tolmetin can also increase the risk of gastrointestinal conditions such as perforation or
bleeding, which is fatal.
• Antacids can be taken with Tolmetin to relieve stomachaches that often occur.
• Overdose can result in drowsiness, nausea, epigastric pain, and vomiting.

2.8 Zomepriac

IUPAC NAME: 2-[5-(4-chlorobenzoyl)-1,4-dimethyl pyrrol-2-yl] acetic acid

Therapeutic Uses
 • Zomepirac was indicated for the management of mild to severe pain.
• Multiple clinical trials demonstrated zomepirac to be more effective than aspirin or
codeine alone and to be as effective as analgesic combinations containing codeine or
other opioids.

Adverse Effects

• Zomepirac is associated with an increased incidence of urogenital symptoms such as

dysuria and pyuria.
• Because of tumorigenicity in rats, the drug is contraindicated in children, pregnant
women, and nursing mothers.

2.9 Diclofenac

IUPAC NAME: 2-[(2, 6-Dichlorophenyl) amino] phenyl-acetate

Therapeutic Uses

• Diclofenac is used to treat pain, inflammatory disorders, and dysmenorrhea.

Adverse Effects

• Indigestion, gas, stomach pain, nausea, vomiting.

• Diarrhea, constipation.
• Headache, dizziness, drowsiness.
• Stuffy nose.
• Itching increased sweating.
• Increased blood pressure.
• Swelling or pain in your arms or legs.

2.10 Ketorolac
IUPAC NAME: 5-benzoyl-2, 3-dihydo-1H-pyrrolizine-1-carboxylic acid
Therapeutic Uses:-
• Ketorolac is used for short-term management of moderate to severe pain.
• It is usually not prescribed for longer than five days, due to its potential to cause kidney
damage.
• Ketorolac is effective when administered with paracetamol to control pain in newborns
because it does not depress respiration as do opioids.
• Ketorolac is also an adjuvant to opioids medications and improves pain relief.

Adverse Effects:-
• Headache.
• Drowsiness.
• Indigestion.
• Stomach or abdominal pain.

2.11 Ibuprofen
IUPAC NAME(RS)-2-(4-Isobutyl phenyl) Propionic acid

Therapeutic Uses:-
• Ibuprofen is used primarily to treat fever (including post-vaccination fever), mild to
moderate pain (including pain relief after surgery), painful menstruation, osteoarthritis,
dental pain, headaches, and pain from kidney stones.
• About 60% of people respond to any NSAID; those who do not respond well to a
particular one may respond to another.
• It is used for inflammatory diseases such as juvenile idiopathic arthritis and rheumatoid
arthritis.
Adverse Effects:-
• upset stomach, mild heartburn, nausea, vomiting;
• bloating, gas, diarrhea, constipation;
• dizziness, headache, nervousness;
• decreased appetite;
• mild itching or rash; or.

2.12 Naproxen
IUPAC NAME : 2-(6-Methoxy-2-naphthyl) Propionic acid

Therapeutic Uses:-
• Naproxen's medical uses are related to its mechanism of action as an anti-inflammatory
compound.
• Naproxen is used to treat a variety of inflammatory conditions and symptoms that are
due to excessive inflammation, such as pain and fever (naproxen has fever-reducing,
or antipyretic, properties in addition to its anti-inflammatory activity).
• Notably, not all medications that reduce fever are anti-inflammatory compounds (such
as paracetamol).
Adverse Effects:-
• indigestion, heartburn, stomach pain, nausea;
• headache, dizziness, drowsiness;
• bruising, itching, rash;
• swelling; or.
• ringing in your ears.

2.12 Piroxicam
IUPAC NAME: 4-Hydroxy-2-methyl-N-(2-pyridinyl)2H-1, 2-benzothiazine-3-carboxamide 1,1-
dione

Therapeutic Uses:-
• It is used in the treatment of rheumatoid and osteoarthritis, primary dysmenorrhea,
postoperative pain; and act as an analgesic, especially where there is
an inflammatory component.
• The European Medicines Agency issued a review of its use in 2007 and recommended
that its use be limited to the treatment of chronic inflammatory conditions, as it is only in
these circumstances that its risk-benefit ratio proves to be favorable.
Adverse Effects:-
• abnormal liver function tests;
• urination problems;
• upset stomach, heartburn, loss of appetite, stomach pain, nausea, vomiting;
 • gas, diarrhea, constipation.

2.13 Phenacetin
IUPAC NAME: N-(4-Ethoxy phenyl) acetamide

Therapeutic Uses:-
• Phenacetin has been used as a cutting agent to adulterate cocaine in the UK and Canada,
due to the similar physical properties.
• Due to its low cost, phenacetin is used for research into the physical and refractive
properties of crystals. It is an ideal compound for this type of research.
Adverse Effects:-
• In the United States, the Food and Drug Administration ordered the withdrawal of drugs
containing phenacetin in November 1983, due to its carcinogenic and kidney-damaging
properties.

2.14 Acetaminophen
IUPAC NAME: 4-Hydroxy acetanilide

Therapeutic Uses:-
• Acetaminophen is an analgesic used to temporarily relieve minor aches and pains due
to headache, muscular aches, backache, minor pain of arthritis, the common
cold, toothache, and premenstrual and menstrual cramps.
• Acetaminophen is also used to temporarily reduce fever.
Adverse Effects:-
• Nausea, vomiting, loss of appetite, or severe stomach pain.
• Trouble passing urine or change in the amount of urine.
• Light-headedness, sweating, fainting, or weakness.
• Unusual bruising or bleeding.
2.15 Antipyrine
IUPAC NAME: 2,3-Dimethyl-1-phenyl-3-pyrazolin-5-one
Therapeutic Uses:-
• Antipyrine and benzocaine otic is used to relieve ear pain and swelling caused by
middle ear infections.
• It may be used along with antibiotics to treat an ear infection. It is also used to help
remove a buildup of ear wax in the ear.
• Antipyrine and benzocaine are in a class of medications called analgesics.

Adverse Effects:-

• Allergy to pyrazolones
• Nausea
• Agranulocytosis
• Hepatotoxicity

2.16 Phenylbutazone

IUPAC NAME: 4-Butyl-1,2-diphenyl pyrazolidine-3,5-dione

Therapeutic Uses:-
• Phenylbutazone is a nonsteroidal anti-inflammatory drug (NSAID) effective in treating
fever, pain, and inflammation in the body.
• As a group, NSAIDs are non-narcotic relievers of mild to moderate pain of many causes,
including injury, menstrual cramps, arthritis and other musculoskeletal conditions.
Adverse Effects:-
• Overdose or prolonged use can cause gastrointestinal ulcers, blood
dyscrasia, kidney damage (primarily dose-dependent renal papillary necrosis), oral
lesions if given by mouth, and internal hemorrhage.
• This is especially pronounced in young, ill, or stressed horses which are less able to
metabolize the drug.
• Effects of gastrointestinal damage include edema of the legs and belly secondary to
leakage of blood proteins into the intestines, resulting in decreased appetite, excessive
thirst, weight loss, weakness, and in advanced stages, kidney failure and death.

✓ Learning Outcome:-
1. Understand the chemistry of drugs with respect to their pharmacological activity.
 2. Know the Structural Activity Relationship (SAR) of different class of drugs.

Narcotic and Non-Narcotic Analgesics

Introduction
Narcotics are addictive drugs that reduce the user's perception of pain and induce euphoria (a
feeling of exaggerated and unrealistic well-being). The English word narcotic is derived from the
Greek narkotikos , which means "numbing" or "deadening." Although the term can refer to any
drug that deadens sensation or produces stupor, it is commonly applied to the opioids—that is, to
all natural or synthetic drugs that act like morphine.

Classification
Mechanism of action

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), were defined
pharmacologically several years ago. Recently, the 3 opioid receptors have been cloned, and
their molecular structures described. These receptors belong to the large family of receptors
which possess 7 transmembrane-spanning domains of amino acids.

Pharmacological studies have shown that the naturally -occurring opioid peptide, b endorphin,
interacts preferentially with m receptors, the enkephalins with d receptors and dynorphin with k
receptors . Morphine has considerably higher affinity for m receptors than for other opioid
receptors. The opioid antagonist, naloxone, inhibits all opioid receptors, but has highest affinity
for m receptors. All 3 receptors produce analgesia when an opioid binds to them. However,
activation of k receptors does not produce as much physical dependence as activation of m
receptors.

1. Morphine sulphate
IUPAC NAME:7,8-didehydro-4,5-epoxy-17-methyl morphinan-3,6 α diol

Uses:
• Preservative-free Morphine Sulfate Injection is indicated for the management of pain
where use of an opioid analgesic by PCA is appropriate.
• It was developed for administration via a compatible Hospira infusion device.
Adverse Effects:
• The most serious side effect is respiratory depression. Because of delay in maximum
CNS effect with intravenously administered drug (30 min), rapid administration may
result in overdosing.
• The depression may be severe and could require intervention While low doses of
intravenously administered morphine have little effect on cardiovascular stability, high
doses are excitatory, resulting from sympathetic hyperactivity and increase in circulating
catecholamines.

2. Codeine,
IUPAC NAME: 7,8-didehydro-4,5-epoxy-3-methoxy-17-methyl morphinan-6 α-ol

Uses:
• Codeine is used to treat mild to moderate pain and to relieve coughing.
• It is also used to treat diarrhea and diarrhea-predominant irritable bowel
syndrome, although loperamide (which is available without a prescription for
milder diarrhea), diphenoxylate, paregoric, or even laudanum are more frequently
used to treat severe diarrhea.
• Weak evidence indicates that it is useful in cancer pain, but it is associated with
increased side effects.
• The American Academy of Pediatrics does not recommend its use in children due
to side effects. The FDA lists age under 12 years old as a contraindication to use.
Adverse effects:
• Common adverse effects associated with the use of codeine
include drowsiness and constipation.
• Less common are itching, nausea, vomiting, dry mouth, miosis, orthostatic
hypotension, urinary retention, euphoria, and dysphoria.
• Rare adverse effects include anaphylaxis, seizure, acute pancreatitis,
and respiratory depression.
 • As with all opiates, long-term effects can vary, but can include diminished libido,
apathy, and memory loss. Some people may have allergic reactions to codeine,
such as the swelling of skin and rashes.

3. Meperidine hydrochloride
IUPAC NAME: Ethyl-1-methyl-4-phenylpiperidine-4-carboxylate hydrochloride

Uses:
• Pethidine is the most widely used opioid in labour and delivery but has fallen out of
favour in some countries such as the United States in favour of other opioids, due to its
potential drug interactions (especially with serotonergics) and its neurotoxin
metabolite, norpethidine.
• It is still commonly used in the United Kingdom and New Zealand,[15] and was the
preferred opioid in the United Kingdom for use during labour, but has been replaced
largely by hydromorphone since the mid-2000s.[16]
• Pethidine is the preferred painkiller for diverticulitis, because it decreases intestinal
intraluminal pressure.

Adverse effects:
• The major hazards of Meperidine, as with other opioid analgesics, are respiratory depression and,
to a lesser degree, circulatory depression, respiratory arrest, shock, and cardiac arrest.
• The most frequently observed adverse reactions included lightheadedness, dizziness, sedation,
and nausea, vomiting, and sweating.
4. Anilerdine hydrochloride
IUPACNAME: Ethyl-1-[2-(4-aminophenyl)ethyl]-4-phenylpiperidine-4-carboxylate

Uses:
• Anilerdine is a synthetic opioid and strong analgesic medication.
• It is a narcotic pain reliever used to treat moderate to severe pain.
 • Narcotic analgesics act in the central nervous system (CNS) to relieve pain. Some of
their side effects are also caused by actions in the CNS.
Adverse effects:
• Anilerdine is absorbed by all routes of administration.
• Symptoms of overexposure include dizziness, perspiration, a feeling of warmth, dry
mouth, visual difficulty; itching, euphoria, restlessness, nervousness and excitement have
been reported.

5. Diphenoxylate hydrochloride
IUPAC NAME: Ethyl-1-(3-cyano-3,3 diphenyl propyl)-4-phenyl-piperidine-4-
carboxylate hydrochloride

Uses:
• This medication is used to treat diarrhea.
• It helps to decrease the number and frequency of bowel movements. It works by slowing
the movement of the intestines.
• Diphenoxylate is similar to narcotic pain relievers, but it acts mainly to slow the gut.

Adverse effects:
• drowsiness, dizziness, feeling restless;
• headache;
• numbness in your hands or feet;
• depression, not feeling well;
• confusion, feelings of extreme happiness;
• red or swollen gums;
• dry mouth, nose, or throat;
• Nausea, vomiting, upset stomach, loss of appetite.

6. Loperamide hydrochloride
IUPAC NAME 4-[4-(4-chlorophenyl)-4-hydroxypiperidine]-N,N-dimethyl-2,2-
diphenyl butyramide hydrochloride
 Uses:
• This medication is used to treat sudden diarrhea (including traveler's diarrhea).
• It works by slowing down the movement of the gut.
• This decreases the number of bowel movements and makes the stool less watery.
Loperamide is also used to reduce the amount of discharge in patients who have had an
ileostomy.

Adverse effects:
• Dizziness.
• Drowsiness.
• Dry mouth.
• Vomiting.
• Constipation.
• Fatigue.
• Stomach pain, discomfort, or enlargement.
7. Fentanyl citrate
IUPAC NAME: N-phenyl-N-[1-(2-phenylethyl)piperadin-4-yl] propanamide-2-
hydroxy-1,2,3-propane-tricarboxylate

Uses:
• Intravenous fentanyl is often used for anesthesia and to treat pain.
• To induce anesthesia, it is given with a sedative-hypnotic, like propofol or thiopental, and
a muscle relaxant.
• To maintain anesthesia, inhaled anesthetics and additional fentanyl may be used. These
are often given in 15-30 minute intervals throughout procedures such as endoscopy,
surgeries, and in emergency rooms.
Adverse effects:
• Fentanyl's most common side effects, which affect more than 10% of people, include
diarrhea, nausea, constipation, dry mouth, somnolence, confusion, asthenia (weakness),
sweating.
 • Less frequently, in 3-10% of people, fentanyl can cause abdominal pain, headache,
fatigue, anorexia and weight loss, dizziness, nervousness, hallucinations, anxiety,
depression, flu-like symptoms, dyspepsia (indigestion), shortness of
breath, hypoventilation, apnoea, and urinary retention.
• Fentanyl use has also been associated with aphasia. Despite being a more potent
analgesic, fentanyl tends to induce less nausea, as well as less histamine-mediated
itching, than morphine.
8. Methadone hydrochloride
IUPAC NAME: (RS)-Dimethyl (1-methyl-4-oxo-3,3-diphenylhexyl)-amine
hydrochloride

Uses:
• Methadone is used for the treatment of opioid use disorder.
• It may be used as a maintenance therapy or in shorter periods for detoxification to
manage opioid withdrawal symptoms.
• A 2009 Cochrane review found methadone was effective in retaining people in treatment
and in the reduction or cessation of heroin use as measured by self-report and urine/hair
analysis but did not affect criminal activity or risk of death.
• Treatment of opioid-dependent persons with methadone follows one of two routes:
maintenance or detoxification. Methadone maintenance therapy (MMT) usually takes
place in outpatient settings.
Adverse effects:

• Sedation
• Diarrhea or constipation
• Flushing
• Perspiration and sweating
• Heat intolerance
• Dizziness or fainting
• Weakness

9. Propoxyphene Hydrochloride
IUPAC NAME: (1S,2R)-1-Benzyl-3-dimethylamino-2-methyl-1-phenyl propyl
propionate hydrochloride
 Uses
• Propoxyphene is in a group of drugs called narcotic pain relievers.
• Propoxyphene is used to relieve mild to moderate pain.
• Propoxyphene may also be used for purposes other than those listed in this medication
guide.
Adverse effects:
• lightheadedness
• drowsiness
• dizziness
• sleepiness
• constipation

10. Pentazocine
IUPAC NAME: (2RS,6RS, 11RS)-6, 11-dimethyl-3-(3-methyl but-2-enyl)-
1,2,3,4,5,6-hexahydro-2,6-methano-3 benzocin-8-ol

Uses:
• Pentazocine injection is used to relieve moderate to severe pain.
• It may also be used before surgery or with a general anesthetic (medicine that puts you to
sleep).
• Pentazocine belongs to the group of medicines called narcotic analgesics (pain
medicines). It acts on the central nervous system (CNS) to relieve pain.
Adverse effects:
• noisy breathing, sighing, shallow breathing;
• a light-headed feeling, like you might pass out;
• severe constipation;
• pain, burning, irritation, or skin changes where the injection was given.
11. Levorphanol tartarate
IUPAC NAME: (-)-3-hydroxy-N-methyl-morphinan

Uses:
• This medication is used to treat moderate to severe pain.
• Levorphanol is an opioid (narcotic) pain reliever.
• It acts on certain centers in the brain to give you pain relief.
Adverse effects:
• Nausea,
• vomiting, constipation, lightheadedness,
• dizziness, drowsiness, dry mouth,
• Flushing, or vision problems may occur.
• If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
12. Nalorphine hydrochloride
IUPAC NAME: (-)-3-hydroxy-N-methyl-morphinan hydrochloride

nalorphine produces side effects such as dysphoria, anxiety, confusion, and hallucinations, and
for this reason, is no longer used medically.

Levallorphan tartarate
IUPAC NAME: (-)-17-allylmorphinan-3-ol

Uses:
 • Levallorphan was formerly widely used in general anesthesia, mainly to reverse the
respiratory depression produced by opioid analgesics and barbiturates used for induction
of surgical anaesthesia whilst maintaining a degree of analgesia.

Adverse effects:
• Levallorphan can produce severe mental reactions at sufficient doses including
hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety,
confusion, dizziness, disorientation, derealization and feelings of drunkenness.

Naloxone hydrochloride:
IUPAC NAME: 4, 5 α-Epoxy-3, 14-dihydroxy-17-(prop-2-enyl) morphinan-6-one hydrochloride

Uses:
• It is an opioid antagonist used for the complete or partial reversal of opioid overdose,
including respiratory depression.
• Narcan is also used for diagnosis of suspected or known acute opioid overdose and also
for blood pressure support in septic shock.
• Narcan is available in generic form.

Adverse effects:
• nausea, vomiting, diarrhea, stomach pain;
• fever, sweating, body aches, weakness;
• tremors or shivering, fast heart rate, pounding heartbeats, increased blood pressure;
• Feeling nervous, restless, or irritable.

General Anesthetics
Objective:- Inhalation anesthetics: Halothane*, Methoxyflurane, Enflurane, Sevoflurane,
Isoflurane, Desflurane.Ultra short acting barbitutrates: Methohexital sodium*, Thiamylal sodium,
Thiopental sodium. Dissociative anesthetics: Ketamine hydrochloride.*
1. Halothane:-
IUPAC NAME:2-bromo,2-chloro,1,1,1-trifluoroethane

2. Methoxyflurane
IUPAC NAME:2,2-dichloro-1,1-difluoro-1-methoxyethane
3. Enflurane
IUPAC NAME:2-chloro-1,1,2-trifluoroethyldifluoromethylether

4. Sevoflurane
IUPAC NAME:1,1,1,3,3,3-hexafluoro-2-(fluoromethoxy) propane

5. Isoflurane
IUPAC NAME:

6. Desflurane
IUPAC NAME:2-(difluoromethoxy)-1,1,1,2-tetrafluoroethane

7. Methohexital sodium
IUPAC NAME: sodium;5-hex-3yn-2-yl-1-methyl-2,6-dioxo-5-prop-2-enylpyrimidin-4-
olate
 8. Thiamylal sodium
IUPAC NAME:sodium;4,6-dioxo-5-pentan-2-yl-5-prop-2-enyl-1H-pyrimidine-2-
thiolate

9. Thiopental sodium
IUPAC NAME: sodium;5-ethyl-4,6-dioxo-5-pentan-2-yl-1H-pyrimidine-2-thiolate

10. Ketamine hydrochloride

IUPAC NAME:2-(2-chlorophenyl)-2-(methylamino)cyclohexane-1-one
hydrochloride.

Uses of General An aesthetics

Adverse effects of General Anesthetics

Learning outcomes
➢ Students know about the classification, mechanism of action & uses of some drugs.