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7/24/2021

Analgesics
Pharmacist
Marwan Qasim

Pain

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Introduction
• Pain is an unpleasant sensory and emotional
experience associated with actual or potential
tissue damage.

• Pain is not just a physical sensation. It is


influenced by attitudes, beliefs, personality and
social factors, and can affect emotional and
mental wellbeing.

• There are three main categories of pain: acute,


chronic and cancer pain

Types of pain
• Acute pain lasts for a short time and occurs following
surgery or trauma or other condition. It acts as a warning to
the body to seek help. Although it usually improves as the
body heals, in some cases, it may not.

• Chronic pain lasts beyond the time expected for healing


following surgery, trauma or other condition. It can also
exist without a clear reason at all. Although chronic pain
can be a symptom of other disease, it can also be a disease
in its own right, characterised by changes within the central
nervous system.

• Cancer pain can occur in patients with early stage and


advanced disease, and in cancer survivors as a severe and
debilitating side-effect of treatment.

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Analgesics

Anesthetic
NSAIDs Opioids agents Others

Inflammation
• Inflammation is a normal, protective response to
tissue injury caused by physical trauma, noxious
chemicals, or microbiologic agents.

• Inflammation is the body’s effort to inactivate or


destroy invading organisms, remove irritants, and
set the stage for tissue repair.

• When healing is complete, the inflammatory


process usually subsides.

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NSAIDs

Salsalate Diflunisal Aspirin Celecoxib


Fenoprofen Fluribiprofen Naproxen Etoricoxib
Oxaprozin Etodolac indomethacin Parecoxib

Ketorolac Tolmetin Sulindac Rofecoxib


Lumiracoxib
Meloxicam Piroxicam Mefenamic acid
Ibuprofen Ketoprofen Diclofenac
Nabumetone Meclofenamate Zaltoprofen

NSAIDs
• The NSAIDs are a group of chemically dissimilar
agents that differ in their antipyretic, analgesic,
and anti-inflammatory activities.

• Non steroidal anti inflammatory drugs are


classified into two categories:

1) Non selective COX inhibitors.


2) Selective COX 2 inhibitors.

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Indications
1) Rheumatoid Arthritis.
2) Osteoarthritis.
3) Back pain.
4) Fever.
5) Dental pain.
6) Menstrual pain.
7) Renal colic pain
8) Headache.

Adverse effects

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Examples
Generic name Diclofenac Generic name Meloxicam
Mother name Voltaren
Mother name Mobic
Brand name Olfen
Dosage form tablet (25mg, 50mg,
Brand name Loxim, Zeloxim
75mg), extended-
release tablet
(100mg), capsule Dosage form tablet (7.5mg,
(18mg, 25mg, 35mg), 15mg), capsule
powder sachet (5mg, 10mg),
(50mg), ampoule Ampule (15mg).
(75mg), IV solution
(37.5mg),
Suppository (12.5mg,
25mg, 50mg,
100mg).
Doses One to two times
daily
Doses One to two times
daily

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Examples
Generic name Ibuprofen Generic name Mefenamic acid
Mother name Advil
Mother name Ponstan
Brand name Profinal
Dosage form tablet (100mg, Brand name Fendol
200mg, 400mg,
600mg, 800mg), Dosage form capsule (250mg,
capsule (200mg), 500mg), tablet
chewable tablet (250mg, 500mg).
(50mg, 100mg), oral (Oral suspension
suspension 100mg\5ml)
(100mg/5ml,
40mg/ml)
Doses Twice daily.
Doses Three to four times
daily.

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Examples
Generic name Celecoxib Generic name Etoricoxib

Mother name Celebrex Mother name Arcoxia

Brand name Flamex Brand name Orotix, Aroxia

Dosage form capsule (50mg, Dosage form Tablets (60mg,


100mg, 200mg, 90mg, 120mg).
400mg)
oral solution
25mg/mL

Doses One to two times Doses Once daily.


daily.

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Opioids
Weak Moderate Strong
Opioids Opioids Opioids
Propoxephene Tramadol Morphine
Codeine Buprenorphine Hydromorphone
Dihydrocodeine Pentazocine Oxymorphone
Hydrocodone Tapentadol Fentanyl
Oxycodone Nalbuphine Methadone
Meperidine
Levorphanol
Butorphanol
Remifentanil
Sufentanil

Pain signal

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Opioids
• Opioids are a class of drugs naturally found in the opium
poppy plant and that work in the brain to produce a variety
of effects, including the relief of pain with many of these
drugs.

• Opioids are used to block pain signals between the brain


and the body and are typically prescribed to treat moderate
to severe pain. In addition to controlling pain, opioids can
make some people feel relaxed, and\or happy.

• Although the opioids have a broad range of effects, their


primary use is to relieve intense pain, whether that pain
results from surgery, injury, or chronic disease.

• Unfortunately, widespread availability of opioids has led to


abuse of those agents with euphoric properties.

Mechanism of action

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Mechanism of action

Indications
1) Moderate to sever pain.
2) Postoperative pain.
3) Euphoria.
4) Cough.
5) Emesis.
6) Diarrhea.

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Adverse effects

Examples
Generic name Tramadol Generic name Methadone

Mother name Ultram Mother name Dolophine

Brand name Tramadol G.L, Doreta Brand name None

Dosage form tablet (50mg, 100mg, Dosage form injectable solution


200mg), capsule (10mg/mL), tablet
(100mg, 150mg , (5mg, 10mg),
200mg, 300mg), oral dispersible tablet
solution (5mg/mL), (40mg), oral solution
injectable solution (5mg/5mL,
(50mg) 10mg/5mL)
Doses Four times daily. Doses Two to three times
daily.

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Anesthetic agents
Lidocaine Chlorprocaine
Tetracaine Procaine
Benzocaine Cocaine
Proparacaine Prilocaine
Bupivacaine Ropivacaine

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Anesthetic agents
• Topical anesthetics are medicines that numb and
reduce the sensation of pain in the area to which
they are applied. They are available as creams,
ointments, solutions, eye drops, gels or sprays
and may be applied to areas such as the skin,
inside the mouth or throat, in the nose, or in the
eyes.

• Topical anesthetics may be applied to the skin to


relieve pain caused by sunburn or other minor
burns, insect bites, minor cuts, or before dressing
changes when wounds are extensive. They may
also be used prior to vaccination or any other
procedure that requires insertion of a needle.

Mechanism of action

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Indications
1) Burns
2) Sunburn
3) Sore throat
4) Epistaxis
5) Minor cuts.
6) Ophthalmic pain.
7) Dental pain.

Adverse effects
Hypersensitivity
Arteriolar dilation
Hypotension
Blurred vision
Nausea and vomiting

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Examples
Generic name Lidocaine Generic name Tetracaine

Mother name Emla Mother name Tetcaine

Brand name Xylogel, xylophil Brand name Anestocaine

Dosage form Topical cram (2%, 5%, Dosage form powder for injection
10%), spray (10%) (20mg), Eye drops
injectable solution (0.5%)
(10mg, 20mg)

Doses Four times daily. Doses Four times daily

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Others
Paracetamol
Capsiacin
Camphor
Menthol

Paracetamol
• The exact mechanism of acetaminophen is
unknown, but its thought that acetaminophen
inhibits prostaglandin synthesis in the CNS. This
explains its antipyretic and analgesic properties.

• Acetaminophen has less effect on cyclooxygenase


in peripheral tissues which accounts for its weak
anti-inflammatory activity. It is not considered to
be an NSAID.

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Best choice for children and pregnant


women

Capsaicin
• Capsaicin is an active component of chili peppers.

• Capsaicin is used as an analgesic in topical


ointments and dermal patches to relieve pain, It
may be applied in cream form for the temporary
relief of minor aches and pains of muscles and
joints associated with arthritis and backache.

• The burning and painful sensations associated with


capsaicin result from its chemical interaction with
sensory neurons. Capsaicin binds to a receptor
called the vanilloid receptor subtype 1 (TRPV1).

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Effects of capsaicin

Examples
Generic name Acetaminophen Generic name Capsaicin
Mother name Panadol
Mother name Capzacin
Brand name Parrazar, Adol
Dosage form tablet (250mg, Brand name Johnson pathch
500mg), Caplet
(325mg, 500mg,
1000mg), capsule Dosage form Topical ointment
(325mg, 500mg), oral (0.025%, 0.05%,
disintegrating tablet 0.1%), Topical patch
(80mg, 160mg), (.025%, 0.05%, 0.1%)
chewable tablet
(80mg), oral solution
or suspension
(125mg/5ml,
250mg/5ml),
Doses One to two times
Doses Four times daily. daily.

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