Pain Medicine and Anti-inflammatory Drugs in Dentistry

T.3 – Pain Medicine

Analgesics

Analgesics are symptomatic medications that decrease the perception of pain without affecting the underlying cause. They are divided into:

Opioid Analgesics

These medications act on the central nervous system (CNS) to alleviate severe pain.

Non-Opioid Analgesics

These medications act on the peripheral nervous system (PNS) and are the most commonly used in oral pathologies.

Non-Opioid Analgesics

They are divided into:

  • a) Nonsteroidal Anti-inflammatory Drugs (NSAIDs): e.g., Aspirin

  • b) Antipyretics: These have little or no anti-inflammatory activity.

Mechanisms of Action of NSAIDs

NSAIDs exert their analgesic and anti-inflammatory effects by inhibiting the synthesis of prostaglandins, which are mediators of pain and inflammation. They also inhibit the synthesis of the enzyme cyclooxygenase, which converts arachidonic acid into prostaglandins and thromboxanes. The analgesic activity of NSAIDs is of moderate intensity and is less than that of opioid analgesics. They are useful for dental pain, joint pain, muscle pain, headaches, and fever. Prostaglandins influence the increase in body temperature, and NSAIDs suppress this response.

Indications of NSAIDs

NSAIDs are indicated for treating mild to moderate pain.

Adverse Effects of NSAIDs

Chronic treatment with NSAIDs can cause erosions and ulcers in the gastric and duodenal mucosa. Side effects may include:

  • Gastritis

  • Heartburn

  • Diarrhea

  • Constipation

  • Dyspepsia (bad digestion)

Prolonged use can cause:

  • Renal toxicity

  • Hypersensitivity

  • Hematological reactions

Acetylsalicylic Acid (Aspirin)

Properties

  • Analgesic and antipyretic in doses of 0.5 to 2g orally.

  • Anti-inflammatory action in doses from 3g/24h.

  • Platelet antiaggregatory action, which appears even in small doses, by inhibition of platelet cyclooxygenase. Not recommended before and after dental treatment.

  • Action on uric acid secretion. At low doses (1g/24h) produces inhibition of secretion. In high doses (+3 g/24h) promotes it.

Pharmacokinetics of Aspirin

  • It is absorbed in the stomach and first part of the duodenum.

  • It has rapid spread and high capacity tissue binding proteins (80%).

  • Able to move to other weak acidic substances, such as antivitamins K.

Metabolism of Aspirin

Short half-life (15 min.) since it hydrolyzes very rapidly into:

a) Salicylic acid

b) Acetic acid

Dosage

Children: 50mg/kg/24h

Adults: 1 to 3g/24h

Presentation

  • Effervescent tablets

  • Soluble powders

  • Injectable solutions

Aspirin is also associated with other active ingredients:

  • Dolmen

  • Couldina

  • Fiorinal

  • Desenfriol

Unwanted Effects of Acetylsalicylic Acid

  • Heartburn

  • Microhemorrhages

  • Risk of gastroduodenal ulcers

  • Allergic manifestations: (Do not use in asthmatics)

    • Urticaria

    • Erythema

    • Anaphylactic shock

  • Blood dyscrasias: Due to antiplatelet action. Aspirin can be used to prevent thrombosis, the origin of cardiovascular and cerebral events.

  • Hemolytic anemia

In cases of overdose, symptoms include: Vertigo, tinnitus (hearing noises), dehydration, respiratory problems, convulsions, and coma. It is important to respect the doses and distribute them regularly during the day.

Contraindications

  • Gastroduodenal pathology

  • Blood dyscrasias

  • History of allergy to aspirin

  • Do not give aspirin to patients taking Sintrom (or other anticoagulants)

Antipyretics with Little or No Anti-inflammatory Activity

1) Paracetamol

Paracetamol is an analgesic and antipyretic that is effectively similar to aspirin but has no anti-inflammatory action.

Pharmacokinetics of Paracetamol
  • Rapid gastrointestinal absorption

  • Good tissue dissemination

  • Hepatic metabolism

  • Renal excretion

Presentation and Dosage
  • Available in the form of suppositories for infants, children, and adults.

  • Available in the form of powders, tablets, and injectables (e.g., Efferalgan, Termalgin).

Dosage
  • Children: 20mg/kg/24h (split into 3 or 4 doses)

  • Adults: 1 to 3 g/24h

Can be used in patients with hemophilia or bleeding, as it does not decrease platelet aggregation. Its main side effect is liver toxicity. It is the analgesic of choice for mild or moderate pain in children under 12 years to avoid Reye’s syndrome (a multisystemic disease that occurs in children under 12 years).

2) Metamizole (Dipyrone) (Nolotil)

Metamizole is a potent analgesic. A dose of 2g can match the effect of low doses of opioids. It acts on smooth muscle and is useful in colic pains. It is an effective analgesic in the treatment of moderate pain and is especially suited for intramuscular injection. It has strong antipyretic properties and little activity on the gastric mucosa and platelet aggregation.

Opioid Analgesics

Opium is obtained from the Asian poppy Papaver somniferum and contains several substances, the most important of which are morphine and codeine. Opioids have analgesic activity and act on specific receptors in the CNS. These painkillers can be:

  • Opium derivatives (morphine, codeine)

  • Synthetic (heroin, methadone, hydrocodone)

Opioid analgesics have a ceiling effect, meaning that the higher the dose, the greater the analgesia. In contrast, with non-opioids, exceeding a certain dose does not increase the analgesic effect.

Mode of Action of Opiates

Opioids interact with receptors in the brain and spinal cord to suppress pain sensation.

Classification of Opioids

  • Agonists: Morphine, Heroin, Codeine, Hydromorphone, Methadone, Fentanyl

  • Antagonists: Naloxone, Naltrexone

Antagonists block the action of the agonists.

Indications of Opioids

Opioid analgesics are indicated for the treatment of severe pain and some types of neuropathic pain. They produce selective analgesia without altering the state of consciousness, vision, or hearing. The duration of effect depends on:

  • Dose

  • Tolerance

  • Characteristics of pain

  • Personality of the patient

Adverse Effects

Morphine-type opiate agonists can cause:

  • Drowsiness

  • Euphoria

  • Miosis (pupil constriction)

  • Nausea and vomiting

  • Constipation

  • Dry mouth

  • Urinary retention

  • Sedation

  • Confusion

  • Acute intoxication with these drugs can produce convulsions, respiratory depression, and cardiovascular collapse. An overdose is treated with naloxone (antagonist).

Morphine

Properties

  • Analgesic effect

  • Produces euphoria and hallucinations

  • Effect on central respiratory system – Respiratory depression and antitussive action

  • Other effects: Constriction of the smooth muscle fibers of the sphincters (constipation), bronchoconstriction, miosis, nausea

Pharmacokinetics

  • Parenteral administration takes 4 hours to take effect.

  • Gastrointestinal absorption is irregular and varies according to individuals.

  • It is recommended that regular administration of morphine be in sweetened preparations, drinkable ampoules, or tablets (for severe pain in cancer patients).

  • Metabolism is hepatic, and elimination is via the bile and saliva.

Dosage

Dosage should be tailored to each patient.

Undesirable Effects

  • Nausea

  • Hypotension

  • Constipation

  • Respiratory depression

The most serious undesirable effect is drug dependence, as it is both psychological and physical. Abstinence syndrome can occur in cases of abrupt discontinuation. Tolerance leads to a dose increase to achieve the desired effect.

Codeine

Codeine is a natural alkaloid of opium with a structure similar to morphine. It is an antitussive and analgesic. It is often used in association with non-opioid analgesics, e.g., Termalgin Codeine.

The undesirable effects are very similar to those of morphine, the most important being constipation, bronchospasm, dizziness, nausea, and drowsiness.

Contraindications

Do not administer to patients with:

  • Respiratory failure

  • Pregnant or breastfeeding women

  • Children

T.3.b – Anti-inflammatory Drugs

Glucocorticoids (Suitable for Extractions)

Glucocorticoids inhibit prostaglandin synthesis at an earlier stage than NSAIDs and have an immunosuppressive effect. In dentistry, they have a very restricted use:

  • Prophylaxis of post-inflammation of 3rd molar extraction (impacted)

  • Autoimmune conditions (lupus, erosive lichen planus, etc.)

  • Allergic reactions (anaphylactic shock, edema of the glottis, etc.)

Drugs

  • Dexamethasone

  • Hydrocortisone

  • Prednisolone

Precautions for Use

  • In patients with ulcers, administer with a gastric protective.

  • Use in diabetic and hypertensive patients can be problematic, causing fluid and sodium retention.

  • May increase anticoagulant effects when given with aspirin, as it increases the level of acetylsalicylic acid in the blood, provoking salicylism.

  • Treatment should not be discontinued abruptly, as this can cause adrenal insufficiency.

  • Long-term treatments can result in psychiatric problems.

Contraindications

Absolute
  • Fungal infections (decrease defenses)

  • Hypersensitivity reactions to steroids

Relative
  • Diabetes, hypertension, osteoporosis, peptic ulcer, psychiatric history