Name of the Opioid Agonist Antagonist Drugs
- Buprenorphine
- Butorphanol
- Nalbuphine
- Pentazocine
| Buprenorphine |
| Availability: Buccal Film: 75 mcg, 150 mcg, 300 mcg, 450 mcg, 600 mcg, 750 mcg, 900 mcg. Implant: Set of 4 implants, each containing 74.2 mg of buprenorphine (equivalent to 80 mg of buprenorphine hydrochloride). Injection Solution: 0.3 mg/1 mL. Tablets, Sublingual: 2 mg, 8 mg. Transdermal Weekly Patch: 5 mcg/hr, 7.5 mcg/hr, 10 mcg/hr, 15 mcg/hr, 20 mcg/hr. |
| Administration/handling: IV Reconstitution: May be diluted with lactated Ringer’s solution, D5W, 0.9% NaCl. Rate of administration: If given as IV push, administer over at least 2 min. IM: Give deep IM into large muscle mass. |
| Buccal Film: Moisten inside cheek. Apply with dry finger. Press and hold in place for 5 sec. Keep film in place until dissolved (approx 30 min). Do not chew, swallow, touch, or move film. Do not cut/tear. Avoid areas with open sores/lesions. |
| Sublingual: Instruct pt to dissolve tablet(s) under tongue; avoid swallowing (reduces drug bioavailability). • For doses greater than 2 tablets, either place all tablets at once or 2 tablets at a time under the tongue |
| Storage: Store parenteral form at room temperature. • Protect from prolonged exposure to light. • Store tablets at room temperature. |
| Transdermal: Apply to clean, dry, intact, non -irritated, hairless skin of upper outer arm, upper chest, upper back, or side of chest. Hair at application site should be clipped; do not shave. • Clean site with clear water and allow to dry. Do not use soaps, alcohol, oils (may increase absorption). Press patch in place and hold for 15 seconds. • Wait minimum of 21 days before reapplying to same site. • Avoid exposing patch to external heat sources. Incidental exposure to water is acceptable. Patch may be taped in place with first-aid tape. • If patch falls off during 7-day dosing interval, apply new patch to a different skin site. |
| Opioid Dependence Sublingual: Adults, children 13 yrs and older: 8 mg on day 1, then 16 mg on day 2 and subsequent induction days. Range: 12–16 mg/day (usually over 3–4 days). Maintenance: Target dose 12–16 mg/day. Pts should be switched to buprenorphine/naloxone combination for maintenance and unsupervised therapy. Implant: Four implants inserted sub-dermally in upper arm for 6 months of treatment. |
| Moderate to Severe Acute Pain IM/IV: Adults, elderly, children 13 yrs and older: 0.3 mg (1 mL) q6–8h prn; may repeat once 30–60 min after initial dose. Children 2–12 yrs: 2–6 mcg/kg q4–6h PRN. |
| Moderate to Severe Chronic Pain: Transdermal: Adults, elderly: (opioid naïve): Initial dose 5 mcg/hr once q7days. (opioid experienced): Discontinue all other around-the-clock opioid medications. Initial dose based on morphine equivalent dose: (Less than 30 mg): Initially 5 mcg/ hr q7days. (30–80 mg): 10 mcg/hr q7days. (Greater than 80 mg): 20 mcg/hr q7days. |
| Buccal: Adults, elderly: (opioid naive): Initially, 75 mcg once or q12h for 4 days, then 150 mcg q12h. (Opioid experienced): Taper current opioid to no more than 30 mg oral morphine equivalent. Based on opioid dose before tapering: 75 mcg once daily or q12h for less than 30 mg; 150 mcg q12h for 30–89 mg; 300 mcg q12h for 90–160 mg. |
Mechanism of Action:
Binds to mu opioid receptors within CNS. Therapeutic Effect: Suppresses opioid withdrawal symptoms, cravings. Alters pain perception, emotional response to pain.
Indications:
- Sublingual tablet: Treatment of opioid dependence.
- Implant: Maintenance treatment of opioid dependence in pts who achieved/sustained prolonged clinical stability on low to moderate doses of a transmucosal buprenorphine product for 3 months or longer with no need for supplemental dosing or adjustments.
- Injection: Relief of moderate to severe pain.
- Transdermal, buccal film: Moderate to severe chronic pain requiring continuous around-the-clock opioid analgesic for extended period.
- OFF-LABEL: Injection: Heroin/opioid withdrawal in hospitalized pts.
Cautions & Contraindications:
- Hypersensitivity
- Significant respiratory depression
- Severe asthma in an unmonitored setting or in absence of resuscitative equipment
- Known or suspected GI obstruction, including paralytic ileus.
- Cautions: Hepatic/renal impairment, elderly, debilitated, pediatric pts, head injury/increased intracranial pressure, pts at risk for respiratory depression, hyperthyroidism, myxoedema, adrenal cortical insufficiency (e.g., Addison’s disease), urethral stricture, CNS depression, morbid obesity, toxic psychosis, prostatic hypertrophy, delirium tremens, kyphoscoliosis, biliary tract dysfunction, acute pancreatitis, acute abdominal conditions, acute alcoholism, pts with prolonged QT syndrome, concurrent use of antiarrhythmics.
Metabolism and Half-life:
Excreted primarily in faeces, with lesser amount eliminated in urine.
Protein binding: High.
Half-life: Parenteral: 2–3 hrs; Sublingual: 37 hrs (increased in hepatic impairment)
Drug Interactions:
- CNS depressants, MAOIs may increase CNS or respiratory depression, hypotension.
- CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole, ritonavir) may increase plasma concentration.
- HERBAL: Herbals with sedative properties may increase CNS depression.
- St. John’s wort may decrease concentration/effect.
SIDE EFFECTS:
- Sedation
- Dizziness
- Nausea, vomiting
- Headache
- Pruritus at application site
- Rash
- Constipation, dry mouth.
- Implant: headache, nausea, vomiting, constipation
- Overdosage results in cold, clammy skin, weakness, confusion, severe respiratory depression, cyanosis, pinpoint pupils, seizures, extreme drowsiness progressing to stupor, coma.
NURSING CONSIDERATIONS
Baseline assessment
- Obtain baseline B/P, pulse rate.
- Assess mental status, alertness.
- Assess type, location, intensity of pain. Obtain history of pt’s last opioid use.
- Assess for early signs of withdrawal symptoms before initiating therapy.
Intervention/evaluation
- Monitor for change in respirations, B/P, rate/quality of pulse, mental status.
- Assess lab results.
- Initiate deep breathing, coughing exercises, particularly in pts with pulmonary impairment.
- Assess for clinical improvement, record onset of relief of pain.
- Monitor strictly for compliance, signs of abuse or misuse.
Patient/family teaching
- Change positions slowly to avoid dizziness, orthostatic hypotension.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Avoid alcohol, sedatives, antidepressants, tranquilizers.
| Butorphanol |
| Availability : Injection: 1 mg/ml, 2 mg/ml Nasal spray: 10 mg/ml |
| Administration and Handling: Make sure solution is clear and free of particulates before giving. •When using nasal spray, insert tip of the sprayer about 1⁄4″ into nostril, point tip backwards, and administer one spray. • Be aware that I.V. route is preferred for severe pain. |
| Moderate to severe pain : Adults: 1 to 4 mg I.M. q 3 to 4 hours as needed, not to exceed 4 mg/dose. Or0.5 to 2 mg I.V. q 3 to 4 hours as needed. With nasal spray, 1 mg (one spray in one nostril) q 3 to 4 hours, repeated in 60 to 90 minutes if needed. |
| Labor pains: Adults: 1 to 2 mg I.V. or I.M., repeated after 4 hours as needed |
| Preoperative anesthesia : Adults: 2 mg I.M. 60 to 90 minutes before surgery |
| Balanced anaesthesia: Adults: 2 mg I.V. shortly before anaesthesia induction, or 0.5 to 1 mg I.V. in increments during anaesthesia |
Mechanism of Action:
Alters perception of and emotional response to pain by binding with opioid receptors in brain, causing CNS depression. Also exerts antagonistic activity at opioid receptors, which reduces risk of toxicity, drug dependence, and respiratory depression.
Metabolism and Half-Life:
Metabolized in Liver. Half-life: 4.6 hr; Duration: 3-4 hr (IV/IM); 4-5hr (nasal)
Excretion: Urine
Indications:
- Pain
- Balanced Anesthesia
- Labor Pain
- Preoperative & Pre-anaesthesia
Cautions & Contraindications:
- Opiate-dependent patients who have not been detoxified
- Acute respiratory depression
- Pregnancy
- Hypersensitivity
- Use cautiously in: head injury, ventricular dysfunction, coronary insufficiency, respiratory disease, renal or hepatic dysfunction, history of drug abuse.
Drug Interactions:
- CNS depressants: additive CNS effects
- Drugs-herbs. Kava, St. John’s wort, valerian: increased CNS depression
- Drug-behaviours. Alcohol use: additive CNS effects
Side- Effects :
- Sedation
- Dizziness, Drowsiness
- Physical dependence, with or without psychological dependence.
- Dyspnea, Diaphoresis
- Confusion, Headache
- Nausea, vomiting
- Constipation
- Hallucinations, mental depression
- HTN and paradoxical CNS excitation (especially in children)
- Rash
- Syncope, tinnitus, vertigo
- Withdrawal syndrome.
- Potentially fatal: respiratory depression, convulsions.
Nursing considerations
Assessment
- History: Hypersensitivity; physical dependence on a narcotic analgesic; pregnancy, lactation
- Bronchial asthma, COPD, increased intracranial pressure
- Acute MI, ventricular failure, coronary insufficiency, hypertension
- Biliary tract surgery, renal or hepatic impairment
- Physical: Orientation, reflexes, bilateral grip strength, affect; pupil size, vision; pulse, auscultation, BP; R, adventitious sounds; bowel sounds, normal output; LFTs, renal function tests
Interventions
- Ensure that opioid antagonist facilities for assisted or controlled respiration are readily available during parenteral administration.
- Monitor respiratory status closely, especially after I.V. administration.
- Watch for signs and symptoms of withdrawal in long-term use and in opioid-dependent patients.
- Assess elderly patient closely for sensitivity to drug.
Patient and Family Teaching:
- Teach patient how to use nasal spray properly.
- Emphasize importance of using drug exactly as prescribed.
- Caution patient that drug may be habit-forming.
- Advise patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and behaviours mentioned above.
- Make them aware of these side effects: Dizziness, sedation, drowsiness, impaired visual acuity (avoid driving, performing other tasks that require alertness); nausea, loss of appetite (lie quietly, eat frequent small meals).
- Report severe nausea, vomiting, palpitations, shortness of breath or difficulty breathing, nasal lesions or discomfort (nasal spray).
| Nalbuphine |
| Availability : Injection Solution: 10 mg/mL, 20 mg/mL. |
| Administration/handling: IV Reconstitution • May give undiluted. Rate of administration • For IV push, administer each 10 mg over 3–5 min. Storage: Store parenteral form at room temperature. IM/SC: Rotate injection sites. • Administer undiluted. |
| Analgesia IV, IM, SC: Adults, elderly: 10 mg q3–6h as needed. Do not exceed maximum single dose of 20 mg or daily dose of 160 mg. Children 1 yr and older: 0.1– 0.2 mg/kg q3–4h as needed. Maximum: 20 mg/dose, 160 mg/day |
| Anaesthesia Supplement: 0.3-3 mg/kg IV over 10-15 minutes, then 0.25-0.5 mg/kg PRN |
Mechanism of Action:
Agonist of kappa opioid receptors and partial antagonist of mu opioid receptors within CNS, inhibiting ascending pain pathways. Therapeutic Effect: Alters pain perception, emotional response to pain.
Indications:
- Relief of moderate to severe pain.
- OFFLABEL: Opioid-induced pruritus.
Cautions & Contraindications:
- Hypersensitivity
- Severe respiratory depression
- Acute or severe bronchial asthma
- GI obstruction including paralytic ileus.
- Cautions: Hepatic/renal impairment, respiratory depression, recent MI, recent biliary tract impairment, pancreatitis, hypovolemia, head trauma, increased intracranial pressure (ICP), pregnancy, pts suspected of being opioid dependent, obesity, thyroid dysfunction, prostatic hyperplasia, urinary stricture, adrenal insufficiency, cardiovascular disease, elderly pts, debilitated pts.
Metabolism & Half – life:
Well absorbed after IM, SQ administration. Metabolized in liver. Primarily eliminated in feces by biliary secretion. Half-life: 3.5–5 hrs.
Drug Interactions:
DRUG: Alcohol, other CNS depressants may increase CNS depression.
HERBAL: Herbals with sedative properties may increase CNS depression
Side effects:
- Sedation
- Diaphoresis, cold/clammy skin
- Nausea, vomiting
- Dizziness, vertigo
- Dry mouth
- Headache
- Abrupt withdrawal after prolonged use may produce symptoms of narcotic withdrawal (abdominal cramping, rhinorrhoea, lacrimation, anxiety, fever, piloerection [goose bumps]).
NURSING CONSIDERATIONS
Baseline assessment
- •Question medical history as listed in precautions.
- •Obtain vital signs before giving medication. If respirations are 12/ min or less (20/min or less in children), withhold medication, contact physician.
- •Assess onset, type, location, duration of pain. Effect of medication is reduced if full pain recurs before next dose.
Intervention/evaluation
- •Monitor for change in respirations, B/P, rate/quality of pulse.
- •Monitor daily pattern of bowel activity, stool consistency.
- •Initiate deep breathing, coughing exercises, particularly in pts with pulmonary impairment.
- •Assess for clinical improvement, record onset of relief of pain.
- •Consult physician if pain relief is not adequate.
Patient/family teaching
- Avoid alcohol.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- May cause dry mouth.
- May be habit forming
| Pentazocine |
| Availability : Injection: 30 mg/ml (as lactate salt) Tablets: 50 mg pentazocine and 0.5 mg naloxone (Talwin NX); 25 mg pentazocine and 650 mg acetaminophen(Talacen) |
| Administration and Handling: Administer each 5-mg I.V. dose by slow direct infusion over 1 minute, with patient lying supine. Use subcutaneous route only when necessary (may cause tissue damage). |
| Moderate to severe pain: preoperative or preanesthetic medication; adjunct to surgical anesthesia Adults: 30 mg subcutaneously, I.M., or I.V. q 3 to 4 hours (not to exceed 60 mg/dose subcutaneously or I.M., or 30 mg/dose I.V.).Maximum daily dosage is 360 mg. |
| Moderate to severe pain :Adults: Initially, one tablet (Talwin Nx) q 3 to 4 hours, increased to two tablets p.r.n., up to a maximum of 12 tablets daily |
| Mild to moderate pain : Adults: One tablet (Talacen) P.O. q 4 hours; up to a maximum of six tablets daily |
| Labor: Adults: 20 mg I.V. for two or three doses at 2- to 3-hour intervals, or 30 mg I.M. as a single dose |
Mechanism of Action
Binds with opioid receptors, mainly kappa and sigma receptors, at many CNS sites to alter perception of and emotional response to pain.
Indications:
- To relieve moderate to severe pain
- To relieve obstetric pain
Cautions & Contraindications:
- Hypersensitivity to pentazocine or its components
- Use cautiously in head trauma, increased intracranial pressure, respiratory conditions, adrenal insufficiency, seizure disorder, acute CNS manifestations, hepatic impairment, acute myocardial infarction, alcohol or narcotic use
- Sulfite sensitivity (talacen)
- History of drug abuse
- Pregnant or breastfeeding patients
Metabolism and Half-life :
- P.O: onset :15-30 min; Peak: 1-3 hr Duration: 3 hr (Talwin NX)
- P.O: onset 15-30 min; peak: 60-90 min Duration: 3 hr (Talacen)
- I. V: onset: 12-30 min; duration: 3 hr: I.M: Onset: 15-20 min; Peak: 15-60 min; duration: 3 hr
Drug interactions:
- Barbiturates, first-generation (sedating) antihistamines, other sedating drugs: additive CNS depression
- MAO inhibitors: unpredictable reactions
- Opioids: decreased analgesic effects
- Alcohol use: increased CNS depression
Side – Effects:
- Chills, dizziness, headache, insomnia, light-headedness, nightmares, paraesthesia, restlessness, weakness
- Hypotension, tachycardia
- Blurred vision, diplopia, dry mouth,
- Laryngeal Edema, laryngospasm
- Constipation, nausea, vomiting
- Decreased urine output
- Atelectasis, bronchospasm, dyspnoea, hypoventilation, wheezing
- Diaphoresis, facial flushing, pruritus, rash,
- Stevens-Johnson syndrome
NURSING CONSIDERATIONS
- Use pentazocine with extreme caution in patients with head injury, intracranial lesion, or increased intracranial pressure.
- Use pentazocine cautiously in patients physically dependent on opioid agonists because drug may prompt withdrawal symptoms; in patients with acute MI because drug’s cardiovascular effects can increase cardiac workload; in patients with renal or hepatic dysfunction because drug is metabolized in liver and excreted in urine; and in patients with respiratory conditions because drug depresses respiratory system.
- When giving repeated parenteral doses, use I.M. or I.V. route when possible and as prescribed because subcutaneous route may cause severe tissue damage at injection site. Rotate I.M. sites to avoid tissue damage.
- After giving parenteral form, expect to taper dosage gradually, as prescribed, to reduce the risk of withdrawal symptoms.
- Monitor vital signs. Watch closely for evidence of shock, dyspnoea, and circulatory or respiratory depression.
- Monitor drug efficacy.
- In prolonged use, assess for signs and symptoms of drug dependence.
Patient And Family Teaching:
- Caution patient that prolonged use of pentazocine may result in dependence.
- Advise patient to avoid driving and hazardous activities until drug’s CNS effects are known.
- Caution patient not to use alcohol or OTC drugs without consulting prescriber.
- Advise patient to report possible allergic reaction, such as a rash or itching.
- Tell patient receiving Talacen or Talwin NX that drug is for oral use only.
- Life-threatening reactions may result from misusing drug by injection.
- Inform patient that withdrawal symptoms may occur if he stops taking drug suddenly after prolonged use.
- Urge patient to avoid alcohol.
- Advise patient to have periodic eye exams.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviours mentioned above.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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