Nalbuphine composition, use, class

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nalbuphine

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Nalbuphine hydrochloride injection prescribing information opioid agonist antagonist indication

Nalbuphine
  • Composition: Nalbuphine hydrochloride, a synthetic opioid of the phenanthrene series. Molecular formula: C₂₁H₂₇NO₃·HCl. It is usually supplied as a sterile injectable solution for IV, IM, or SC use.
  • Class: Mixed opioid agonist-antagonist analgesic. It acts mainly as a kappa (κ) opioid-receptor agonist and a mu (μ) opioid-receptor antagonist/partial antagonist. It has a ceiling effect on respiratory depression. Katzung's Basic and Clinical Pharmacology, 16th Edition describes nalbuphine as a strong κ agonist and partial μ antagonist.
  • Uses:
    • Management of moderate to severe acute pain, including postoperative, traumatic, and obstetric pain
    • Adjunct to balanced anesthesia
    • Sometimes used for opioid-induced pruritus, particularly after neuraxial opioid administration
    • May reduce postoperative shivering in some settings
The DailyMed prescribing information indicates it for pain severe enough to require an opioid when alternatives are inadequate.
Important caution: Because of μ-antagonist activity, nalbuphine can precipitate acute withdrawal in a patient physically dependent on full μ-opioids such as morphine, fentanyl, or heroin. Common adverse effects include sedation, nausea, vomiting, dizziness, sweating, and headache.

Themicaine composition, use, class

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Themicaine medicine composition brand

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Themicaine

Themicaine is a brand of lignocaine (lidocaine), used as a local anesthetic.
ItemDetails
CompositionUsually lignocaine/lidocaine hydrochloride 2%. The jelly contains lignocaine 2% w/v. The plain injection contains lignocaine; some multi-dose formulations also contain preservatives such as methylparaben.
Themicaine ADContains lignocaine hydrochloride 20 mg/mL (2%) + adrenaline/epinephrine 0.005 mg/mL (1:200,000). Adrenaline prolongs local anesthesia and reduces bleeding at the injection site.
ClassAmide-type local anesthetic. Lidocaine also belongs to Class IB antiarrhythmic drugs when given systemically for ventricular arrhythmias, but Themicaine is generally used for local anesthesia.
UsesProduces temporary numbness for minor surgery, suturing, dental procedures, nerve blocks, infiltration anesthesia, and painful mucosal procedures. The jelly formulation can anesthetize skin or mucous membranes, for example before urethral catheterization or certain local procedures.
Use only by the prescribed route and dose. Accidental intravascular injection or excessive use can cause toxicity such as numbness around the mouth, tinnitus, dizziness, seizures, hypotension, or dangerous cardiac rhythm disturbances. The product strengths and excipients vary, so confirm the vial or tube label before administration. The Themicaine 2% product information identifies the jelly as lignocaine 2%, while Themicaine AD information lists lidocaine 20 mg/mL with adrenaline 0.005 mg/mL.

Glycopyrolate composition use class

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glycopyrrolate

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glycopyrrolate injection prescribing information indications anticholinergic composition

Glycopyrrolate
ItemDetails
CompositionActive drug: glycopyrrolate, commonly supplied as glycopyrrolate bromide. Injection is commonly 0.2 mg/mL for IV or IM use.
ClassAnticholinergic (antimuscarinic) drug. It is a quaternary ammonium compound, so it does not significantly cross the blood-brain barrier.
ActionBlocks muscarinic effects of acetylcholine, thereby reducing secretions and vagal effects on the heart.
Uses1. Before anesthesia to reduce salivary, pharyngeal, and tracheobronchial secretions. 2. To prevent or treat vagal reflex bradycardia during anesthesia or surgery. 3. Given with neostigmine during reversal of non-depolarizing neuromuscular blockade, to prevent neostigmine-induced bradycardia and excessive secretions. 4. Oral formulations may be used for chronic severe drooling, especially in children with neurologic disorders. 5. Inhaled glycopyrrolate is used as a long-acting bronchodilator component in some COPD treatments.
In anesthesia, glycopyrrolate is preferred with neostigmine because their durations are similar. It reduces secretions with minimal central nervous system effects because it does not cross the blood-brain barrier. Morgan and Mikhail's Clinical Anesthesiology, 7e.
Common adverse effects: dry mouth, blurred vision, tachycardia, constipation, and urinary retention. Avoid or use carefully in angle-closure glaucoma, urinary retention, and intestinal obstruction. The DailyMed injection label lists its anesthesia-related indications.

Use in a hospital

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glycopyrrolate perioperative

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glycopyrrolate injection hospital use anesthesia neostigmine reversal secretion bradycardia DailyMed

In the hospital, glycopyrrolate injection is used mainly in the operation theatre, recovery room, ICU, and emergency setting:
  1. Before anesthesia and intubation
    • Reduces saliva and airway secretions.
    • Helps provide a drier airway during laryngoscopy, intubation, bronchoscopy, or awake fiber-optic intubation.
    • Reduces vagal reflex bradycardia during airway manipulation.
  2. During surgery
    • Treats or prevents vagally mediated bradycardia, for example due to surgical traction, suctioning, or certain anesthetic drugs.
    • Reduces excessive respiratory tract secretions.
  3. Reversal of muscle relaxation after surgery
    • Given with neostigmine when reversing non-depolarizing neuromuscular blockers.
    • Prevents neostigmine’s muscarinic adverse effects: bradycardia, excess secretions, bronchospasm, and increased bowel activity.
  4. Palliative care / wards
    • May be used to reduce troublesome oral and respiratory secretions in patients who cannot clear them, including terminal respiratory secretions.
  5. Specialist uses
    • To reduce severe drooling (sialorrhea), especially in neurologic disorders.
    • In some hospitals, inhaled formulations are part of maintenance treatment for COPD, not for acute asthma attacks.
It is administered by trained staff with monitoring of heart rate, blood pressure, and secretion status. The official injection information specifically lists reduction of airway secretions, management of vagal-reflex arrhythmias, and protection against neostigmine-related muscarinic effects.
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