Definition Analgesics

Analgesics are drugs /

compounds used for
reducing pain / tenderness
without eliminating
awareness.

Pain is a symptom
which serves to protect and
give an alarm about the presence of
disturbances in the body; like
inflammation, bacteria infections,
and muscle spasms.
 Handling Pain
• Hinder the formation of stimulation on
peripheral pain receptors by peripheral
analgesics.
• Hinder the distribution of stimuli in sensory
nerves, eg with a local anesthetic.
• Blockade of pain centers in the central
nervous system with central analgesics
(narcotics) or with a general anesthetic.
Classification of Pain

1. Acute pain
2. Chronic pain
Analgesics
On the basis of pharmacological, analgesic divided into
two major groups, namely:

1. Peripheral analgesic (non-narcotic), which consists

of drugs that are not narcotic and non-centrally.
2. Narcotic analgesics, specifically used to dispel such
severe pain in cancer.
Peripheral Analgesic

• Not affect the Central Nervous System.

• Not lose consciousness or lead to
addiction.
• Lowering the body temperature in the
state fever.
Mechanism of Action
Mechanism of Action
Peripheral Analgesic

• Paracetamol
• Salicylates: aspirin, salisilamid, and benorilat
• Prostaglandin inhibitors (NSAID'S): ibuprofen
• Pirazolinon derivatives: aminofenazon
• Anthranilic derivatives: mefenamic
• Other: benzidamin
Use
• Analgesic effects
Relieve or eliminate pain without affecting the central nervous system or
lose consciousness, also does not cause addiction (mild to moderate pain
intensity).

• Antipyretic effect
These drugs will lower the body temperature only in the state of fever.
Antipiretiknya power by stimulation of the heat regulating center in the
hypothalamus which results in peripheral vasodilation (in the skin), and
increased spending with heat and sweating a lot.

• Effect of anti-inflammatory or anti-inflammatory

Analgesics also have anti-inflammatory power, especially the NSAID'S
(Non-Steroid Anti-Inflammatory Drugs) including aspirin These substances
are used for pain accompanied by inflammation.
Side Effects
• Side effects The most common disorders
gastrointestinal (salicylate, an inhibitor of
prostaglandin = NSAID'S, derivatives pirazolinon),
damage to blood (paracetamol, salicylates,
derivatives anthranilic, derivatives pirazolinon), liver
and kidney damage (paracetamol, an inhibitor of
prostaglandin), and also allergic skin reaction.
• These side effects occur mainly on the use of old or
in high doses.
Analgesic anti-inflammatory (NSAID'S)

• NSAID'S (Non Steroid Anti Inflamasi Drugs)

efficacious analgesic, antipyretic and anti-
inflammatory properties and is often used to banish
the symptoms of teenage disease, such as arthritis
rheumatica, arthrosis.

• The drug is also effective for other inflammation due

to trauma (a blow, collision, accident). Also on
bruising after surgery or as a result of exercise. The
point of these drugs prevent swelling when taken as
early as possible in high enough doses.
Classification

• Salicylates: aspirin, and diflunisal benorilat

Anti-inflammatory doses 2-3 times higher than the dose of analgesics.
But because the risk of side effects so rarely used in medicine rema.
• Acetate: diclofenac, al diclofenac, indomethacin, sulindac
Aceklofenak rarely used anymore due to cause skin reactions.
Including drug indomethacin strongest anti-inflammatory power. But
more often cause stomach complaints.
• Propionate: Ibuprofen, ketoprofen, naproxen
• Oxicam: piroxicam, tenoxicam, meloxicam
• Anthranilic: mefenamic, nifluminat and meclofenamic acid
• Pyrazolone: (oxy) phenylbutazone, azapropazone
• Other: nabumetone, benzydamine cream 3%, 5% cream bufexamac
Benzidamin anti-inflammatory properties but kkurang effective in
rheumatic disorders.
Mechanism of Action

• The workings of most of the NSAID'S

prostaglandin synthesis by the obstacles which
both types ciklo-oxygenase blocked.

• NSAIDs inhibit'S ideally only ciklo-oxygenase II

/ COX-II (inflammation) and not COX-I
(protection of gastric mucosa).
Side Effects
• Ulcerogenik effects: nausea, vomiting, stomach pain,
gastritis.
• Drugs that cause a lot of serious stomach complaint is
indomethacin, piroxicam.
• Impaired renal function insufficiency, abnormalities in the
regulation of electrolyte and water (edema, hyperkalemia).
Prostaglandins (PG) maintain the volume of blood flowing
through the kidneys (perfusion) due to inhibition of the
synthesis of PG glomeruler perfusion and filtration rate is
reduced by these effects.
• Reduced platelet aggregation, so that the bleeding time
may be extended. This effect is reversible except aspirin.
• Skin reactions: rash and urticaria (diclofenac and sulindac).
• Other: bronkokontriksi, central effects, impaired liver
function (diclofenac).
 NARCORIC ANALGESICS
• Called also OPIOIDA (= resemble opiates) are
substances that work terrhadap typical opioid
receptors in the central nervous system (CNS) to the
perception of pain and the emotional response to
pain changed (reduced).

• The body can synthesize its own opioidnya

substances, ie substances endorphins (endogenous
polypeptide group is contained in the cerebrospinal
fluid (CCS) and can cause effects that mimic the
effects of morphine).
Based Works:

• Opiate agonists
a) Opium alkaloids: morphine, codeine, heroin, morphine nico
b) Substance synthesis: methadone and its derivatives
(propoksifen), pethidine and its derivatives as well as
tramadol.
These drugs work the same way with morphine, differing
only on the potential and long works, side effects and risks
of habituation and addiction.

• Opiate Antagonist: Naloxone, Nalorfin, Pentazocine

Lowering the patient's pain threshold pd yg high pain
threshold.

• Combination
This substance can also bind to the opioid receptors, but
does not activate it works perfectly.
Mechanism of Action
• Endorphins work by occupying the road of pain
receptors in the central nervous system to the feeling
of pain can be blocked.

• Analgesic efficacy of opioids based on its ability to

occupy the remnants of pain receptors are not
occupied by endorphins.

• But when analgesics are used constantly. The

formation of new receptors are stimulated and the
production of endorphins in nerve endings in
rintangi. The result was a habit and addiction.
Use
• Analgesic ladder
WHO has drawn up a program of analgesic use for severe pain
(eg cancer), were classified into 3 classes:
1. Non-opioids:'S NSAIDs, including aspirin and codeine
2. Opioida weak: d-propoksifen, tramadol and codeine or
paracetamol + codeine combination.
3. Opioida strong: morphine and its derivatives as well as the
synthesis of substances opioida.

• First drug ss 4 1 g of paracetamol (4 times daily 1 gram

paracetamol), when the effect is less to 4-6 ss codeine 30-60
mg (with paracetamol). If it is not too strong a new opioida:
morphine (oral, subcutaneous, continuous, IV). The goal of
treatment made ​teresbut above a ladder to avoid the risk of
habituation and addiction to opioida.
Common Side Effects

• CNS suppression, nausea, sedation, depress breathing,

coughing, at higher doses result in decreased mental and
motor activity.
• Gastrointestinal tract: reduced motility (obstipansi),
contraction of the sphincter of the gallbladder (gallstones
colic).
• Urogenital tract: urinary retention (due to increased tone of
the sphincter of the bladder).
• Respiratory tract: bronkokontriksi, breathing becomes more
shallow and frequency down.
• The circulatory system: vasodilatation, hypertension,
bradycardia.
• Habit: the risk of addiction to the use of the old.
Excess and lack of narcotic analgesics

• Morphine, a prototype of this drug, which is available in the form of

injections, by mouth (swallowed) and per-oral sustained release. Slow-
release preparations allow patients free from pain for 8-12 hours and is
widely used to treat chronic pain.
• Opioid analgesics often cause constipation, especially in the elderly.
• Laxative (stimulant laxatives usually, eg senna or phenolphthalein) can
help prevent or treat constipation.
• High doses of opioids often cause drowsiness. To fix can be given
stimulants (eg, methylphenidate).
• Opioid analgesics may aggravate nausea felt by the patient. To overcome
given anti-vomiting drugs, either in the form of per-oral, suppository or
injection (eg, metoclopramide, and prochlorperazine hikroksizin).
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