TarginAct® is a strong pain medicine used for severe pain that needs an opioid analgesic. It is also used to help reduce the risk of constipation linked to opioid treatment.
If you are taking TarginAct®, it is important to understand that it is not an ordinary pain tablet. It contains oxycodone hydrochloride, which is a strong opioid pain-reliever, and naloxone hydrochloride, which is included to help reduce opioid-related constipation. TarginAct® is a prolonged-release tablet, which means it releases the medicine slowly over time.
Quick facts: TarginAct® is taken by mouth, usually twice a day, about 12 hours apart. It must be swallowed whole with enough liquid. Do not break, chew or crush it, because this can release the oxycodone too quickly and may cause a dangerous or possibly fatal overdose.
What it is and what it is used for
TarginAct® contains two active ingredients:
- Oxycodone hydrochloride — a strong opioid pain medicine.
- Naloxone hydrochloride — an opioid receptor blocker included to reduce the risk of constipation.
TarginAct® belongs to a group of medicines called analgesics, which are medicines used for pain relief. In South Africa, it is listed as Schedule 6 (S6).
TarginAct® is used for:
- Treatment of severe pain that requires a strong opioid pain medicine.
- Reducing the risk of constipation linked to opioid treatment.
It is not meant for mild pain. It is also not meant to treat sudden “breakthrough” pain on its own, because it is a prolonged-release medicine.
How it works
TarginAct® works in two linked ways.
The oxycodone part attaches to opioid receptors in the brain, spinal cord and other parts of the body. These receptors are involved in how the body feels and responds to pain. By acting on these receptors, oxycodone helps reduce severe pain.
The naloxone part also attaches to opioid receptors, including those in the gut. When taken by mouth, only a very small amount of naloxone reaches the bloodstream. Its role in this combination is to help reduce the constipation that can happen with opioid medicines.
In simple terms, oxycodone helps with severe pain, while naloxone helps lower the chance of opioid-related constipation.
Who should NOT use this medicine
Do not use TarginAct® if you:
- Are allergic or hypersensitive to oxycodone, naloxone, or any of the other ingredients in the tablet.
- Have any condition where opioids should not be used.
- Have severe breathing depression with low oxygen and/or high carbon dioxide levels.
- Have severe chronic obstructive pulmonary disease.
- Have cor pulmonale.
- Have severe bronchial asthma.
- Have paralytic ileus that is not caused by opioids.
- Have moderate to severe liver impairment.
- Have moderate to severe kidney impairment.
- Have rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption, because TarginAct® contains lactose.
Warning: TarginAct® is not recommended for children and adolescents under 18 years of age. Its safety and effectiveness in this age group have not been established.
Warnings and precautions
Breathing problems
The most serious risk with too much opioid medicine is respiratory depression, which means breathing becomes dangerously slow or weak.
You need extra care if you have reduced lung function or any breathing-related condition. TarginAct® must not be used in severe breathing depression, severe chronic obstructive pulmonary disease or severe bronchial asthma.
Seek urgent help if you become unusually sleepy, very difficult to wake, confused, weak, or if your breathing becomes slow or shallow.
Conditions that need special care
Your doctor must take particular care if you are elderly, frail, or have any of the following:
- Opioid-induced paralytic ileus.
- Severely impaired lung function.
- Myxoedema.
- Hypothyroidism.
- Addison’s disease.
- Toxic psychosis.
- Gallstones.
- Enlarged prostate.
- Alcoholism.
- Delirium tremens.
- Pancreatitis.
- Low blood pressure.
- High blood pressure.
- Existing heart or blood vessel disease.
- Head injury, because of the risk of increased pressure inside the skull.
- Epilepsy or a tendency to have convulsions.
- Current or recent use of MAO inhibitors.
If you have mild liver or kidney impairment, TarginAct® must be used with caution. It must not be used if liver or kidney impairment is moderate to severe.
Dependence, tolerance and withdrawal
TarginAct® contains oxycodone, an opioid. With long-term use, your body may get used to it. This is called tolerance, and it may mean a higher dose is needed to get the same pain relief.
Long-term use can also lead to physical dependence. If the medicine is stopped suddenly, withdrawal symptoms may occur. If treatment is no longer needed, your doctor may reduce the dose gradually to lower the chance of withdrawal symptoms.
There is also a risk of psychological dependence or addiction with opioid pain medicines. TarginAct® should be used with particular care if you have a history of alcohol or drug abuse.
TarginAct® is not suitable for treating withdrawal symptoms.
Switching from other opioids
If you have been taking higher doses of other opioids for a long time, switching to TarginAct® may initially trigger withdrawal symptoms. Your doctor may need to monitor you closely during the change.
Do not misuse the tablets
TarginAct® is made for swallowing by mouth only.
Do not inject, snort, crush, chew or dissolve the tablets. Misusing the medicine can cause serious harm. Injecting tablet ingredients may cause tissue damage, lung problems and other serious or potentially fatal effects.
Warning: The tablets must be swallowed whole. Breaking, chewing or crushing them can release the active ingredients too quickly and may lead to absorption of a possibly fatal dose of oxycodone.
Tablet shell in the stool
You may notice what looks like the tablet shell in your stool. This can happen because of the prolonged-release tablet matrix. The source does not state that this means the medicine has not worked.
Surgery
TarginAct® is not recommended before surgery or during the first 12 to 24 hours after surgery.
Cancer-related bowel conditions
TarginAct® is not recommended in patients with cancer associated with peritoneal carcinomatosis or with subocclusive syndrome in advanced digestive and pelvic cancers, because there is no clinical experience in these situations.
Doping tests
TarginAct® may cause positive results in doping controls. Using TarginAct® as a doping agent may be a health hazard.
Driving and using machines
TarginAct® may affect your ability to drive or use machines. This is especially likely:
- When you first start treatment.
- After your dose is increased.
- When changing from another medicine.
- If TarginAct® is taken with alcohol.
- If TarginAct® is taken with other medicines that depress the central nervous system.
Once you are stable on a specific dose, you may not necessarily be restricted from driving or using machines. You should ask your medical practitioner whether it is safe for you to drive or operate machinery.
Alcohol
Alcohol can increase the central nervous system depressant effects of TarginAct®. This may raise the risk of serious effects such as breathing problems. The source specifically warns about combining TarginAct® with alcohol or other central nervous system depressants.
Pregnancy, planning pregnancy, and breastfeeding
TarginAct® is not recommended during pregnancy or labour.
Both oxycodone and naloxone pass through the placenta. Long-term use of oxycodone during pregnancy may lead to withdrawal symptoms in the newborn baby. If oxycodone is given during childbirth, it may cause breathing depression in the newborn.
Oxycodone passes into breast milk. It is not known whether naloxone passes into breast milk. TarginAct® should therefore not be used by mothers who are breastfeeding their infants.
Planning pregnancy is not specifically discussed in the source. Speak to your doctor or pharmacist before using TarginAct® if you are pregnant, planning pregnancy, or breastfeeding.
Interactions
No interaction studies were performed in adults, but the source lists several important possible interactions.
Tell your doctor or pharmacist about all medicines, supplements and herbal products you use, including those bought without a prescription.
Medicines and substances that can increase drowsiness or breathing risk
Substances with central nervous system depressant effects may increase the depressant effects of TarginAct®, including the risk of respiratory depression.
These include:
- Alcohol.
- Other opioids.
- Sedatives.
- Hypnotics.
- Anti-depressants.
- Sleeping aids.
- Phenothiazines.
- Neuroleptics.
- Anti-histamines.
- Anti-emetics.
Warfarin
Changes in INR, also called Quick-value, have been seen when oxycodone and warfarin are used together. These changes may go in either direction.
If you use warfarin, your doctor may need to monitor your blood clotting control carefully.
Anticholinergic medicines
Using oxycodone with anticholinergic medicines, or medicines that have anticholinergic activity, may increase anticholinergic side effects.
Examples mentioned in the source include:
- Tricyclic antidepressants.
- Antihistamines.
- Antipsychotics.
- Muscle relaxants.
- Anti-Parkinson medicines.
Medicines and foods that affect CYP3A4
Oxycodone is mainly processed through a pathway called CYP3A4. Some medicines or foods can slow this pathway down, which may increase oxycodone levels in the blood.
Examples include:
- Macrolide antibiotics, such as clarithromycin.
- Azole antifungal medicines, such as ketoconazole.
- Protease inhibitors, such as ritonavir.
- Grapefruit juice.
Other medicines or herbal products can speed up this pathway, which may lower oxycodone levels in the blood.
Examples include:
- Rifampin.
- Carbamazepine.
- Phenytoin.
- St John’s Wort.
Your TarginAct® dose may need adjustment if these are used together.
Medicines that affect CYP2D6
Some medicines that inhibit CYP2D6 may reduce the clearance of oxycodone and increase oxycodone blood levels.
Examples include:
- Paroxetine.
- Quinidine.
Medicines with minimal expected interaction
The source states that clinically relevant interactions are minimal between therapeutic concentrations of oxycodone/naloxone and:
- Paracetamol.
- Acetylsalicylic acid.
- Naltrexone.
How to take
Step-by-step use
Use TarginAct® exactly as prescribed by your doctor.
- Take it by mouth.
- Swallow the tablet whole.
- Do not break, chew or crush it.
- Take it with enough liquid.
- It may be taken with or without food.
- Take it twice daily according to a fixed schedule.
- For most people, this means taking a dose every 12 hours.
Your doctor will adjust the dose according to your pain level and how sensitive you are to the medicine. The aim is to use the lowest effective dose that gives adequate pain relief.
Note: TarginAct® is a prolonged-release medicine. It is not intended for sudden breakthrough pain.
Starting dose for adults
For an adult who has not used opioids before, the usual starting dose is:
- TarginAct® 10 mg/5 mg every 12 hours.
People who are already using opioids may start on a higher dose, depending on their previous opioid experience. Higher-dose options include TarginAct® 20 mg/10 mg and TarginAct® 40 mg/20 mg.
TarginAct® 5 mg/2,5 mg is used when starting opioid treatment and for individual dose adjustment.
Maximum daily dose
The maximum daily dose of TarginAct® is:
- 80 mg oxycodone hydrochloride
- 40 mg naloxone hydrochloride
Do not take more than prescribed.
Breakthrough pain
If you are taking TarginAct® on a regular schedule, you may still need an immediate-release pain medicine as “rescue” medication for breakthrough pain.
The source states that a single rescue dose should be about one sixth of the equivalent daily dose of oxycodone hydrochloride.
If you need more than two rescue doses per day, this usually means the TarginAct® dose may need to be increased. The source states that dose increases may be made every 1 to 2 days in steps of twice daily 5 mg/2,5 mg, or where needed 10 mg/5 mg, until a stable dose is reached.
Any dose change must be guided by your doctor.
Children and adolescents
TarginAct® is not recommended for anyone under 18 years of age. Safety and effectiveness in this age group have not been established.
Elderly users
For elderly people, the dose is adjusted in the same way as for younger adults, based on pain intensity and individual sensitivity.
Liver or kidney impairment
If you have mild liver impairment, TarginAct® must be used with caution.
If you have moderate or severe liver impairment, TarginAct® must not be used.
If you have mild kidney impairment, TarginAct® must be used with caution.
If you have moderate or severe kidney impairment, TarginAct® must not be used.
Duration of treatment
TarginAct® should not be used for longer than absolutely necessary.
If you need long-term pain treatment, careful and regular monitoring is needed to decide whether ongoing treatment is still necessary.
If opioid treatment is no longer required, your doctor may reduce the dose gradually to help prevent withdrawal symptoms.
Missed dose
Missed dose instructions are not specified in the source. Speak to your doctor or pharmacist for advice on what to do if you miss a dose.
Overdose
An overdose can be serious and may be fatal.
Symptoms linked to oxycodone overdose may include:
- Pinpoint pupils.
- Breathing depression.
- Sleepiness that may progress to stupor.
- Limp or weak muscles.
- Slow heartbeat.
- Low blood pressure.
In severe cases, overdose may cause coma, lung fluid not caused by heart problems, circulatory failure and death.
Symptoms of naloxone overdose alone are unlikely.
Warning: If you think you have taken too much TarginAct®, or if someone else has taken it by accident, seek urgent medical help immediately.
Dosing table
| Age or patient group | Dose | Frequency | Maximum daily dose |
|---|---|---|---|
| Adults who have not used opioids before | 10 mg oxycodone hydrochloride / 5 mg naloxone hydrochloride | Every 12 hours | 80 mg oxycodone hydrochloride / 40 mg naloxone hydrochloride |
| Adults already receiving opioids | May start on higher doses depending on previous opioid experience | Twice daily, according to a fixed schedule | 80 mg oxycodone hydrochloride / 40 mg naloxone hydrochloride |
| Dose titration or individual adjustment | 5 mg oxycodone hydrochloride / 2,5 mg naloxone hydrochloride strength may be used | As prescribed | 80 mg oxycodone hydrochloride / 40 mg naloxone hydrochloride |
| Children and adolescents under 18 years | Not recommended | Not specified in the source | Not specified in the source |
| Elderly patients | Adjust according to pain intensity and individual sensitivity | As prescribed | 80 mg oxycodone hydrochloride / 40 mg naloxone hydrochloride |
Possible side effects
Like all medicines, TarginAct® can cause side effects, although not everyone will get them.
Some side effects may be mild, while others need urgent medical care. Because TarginAct® contains an opioid, breathing-related side effects are especially important.
Common side effects
Common side effects may affect 1% to less than 10% of people.
You may experience:
- Reduced appetite, up to loss of appetite.
- Restlessness.
- Difficulty sleeping.
- Dizziness.
- Headache.
- Sleepiness.
- Abdominal pain.
- Constipation.
- Diarrhoea.
- Dry mouth.
- Indigestion.
- Wind or flatulence.
- Vomiting.
- Nausea.
- Itching.
- Rash.
- Excessive sweating.
- Muscle spasms.
- Muscle twitching.
- Muscle pain.
- Feeling hot and cold.
- Chills.
- Weakness or lack of energy.
- Fatigue.
Diarrhoea may happen as a possible effect of naloxone.
Less common side effects
Less common side effects may affect 0,1% to less than 1% of people.
These may include:
- Hypersensitivity.
- Visual impairment.
- Vertigo.
- Angina, especially in people with a history of coronary artery disease.
- Palpitations linked to withdrawal syndrome.
- Hot flushes.
- Drop in blood pressure.
- Abnormal thinking.
- Anxiety.
- Confusion.
- Depression.
- Reduced libido.
- Euphoric mood.
- Hallucinations.
- Nervousness.
- Convulsions, especially in people with epilepsy or a tendency to convulsions.
- Problems with attention.
- Pins-and-needles sensations.
- Changed sense of taste.
- Speech disorder.
- Fainting.
- Abdominal bloating.
- Burping.
- Increased liver enzymes.
- Erectile dysfunction.
- Urgent need to urinate.
- Shortness of breath.
- Runny nose.
- Cough.
- Chest pain.
- Feeling unwell.
- Pain.
- Weight loss.
- Thirst.
- Injuries from accidents.
Rare and very rare side effects
Rare side effects may affect 0,01% to less than 0,1% of people.
These may include:
- Increased blood pressure.
- Nightmares.
- Medicine dependence.
- Tremor.
- Lethargy.
- Tooth disorder.
- Biliary colic.
- Urinary retention.
- Yawning.
- Weight increase.
Very rare side effects may affect less than 0,01% of people.
These may include:
- Fast heartbeat.
- Sedation.
- Respiratory depression.
Other side effects known for oxycodone
The source also lists additional effects known for oxycodone hydrochloride.
These include:
- Herpes simplex.
- Dehydration.
- Increased appetite.
- Mood and personality changes.
- Reduced activity.
- Psychomotor hyperactivity.
- Agitation.
- Perception disturbances, such as derealisation.
- Aggression.
- Impaired concentration.
- Migraine.
- Increased muscle tone.
- Increased sensitivity to pain.
- Involuntary muscle contractions.
- Reduced sense of touch.
- Abnormal coordination.
- Pinpoint pupils.
- Impaired hearing.
- Widening of blood vessels.
- Voice changes.
- Hiccups.
- Mouth ulcers.
- Inflammation of the mouth.
- Black stools.
- Bleeding gums.
- Dental caries.
- Difficulty swallowing.
- Ileus.
- Cholestasis.
- Dry skin.
- Hives.
- Pain or difficulty passing urine.
- Hypogonadism.
- Absence of menstrual periods.
- Oedema.
- Medicine tolerance.
- Neonatal medicine withdrawal syndrome.
Serious side effects — seek urgent help
Get medical help urgently if you notice signs of serious opioid effects, especially:
- Slow, shallow or difficult breathing.
- Extreme sleepiness or difficulty waking up.
- Collapse, fainting or severe weakness.
- Severe confusion.
- Symptoms of overdose.
- Severe allergic reaction or anaphylactic-type response.
- Convulsions.
- Severe chest pain.
- Signs of withdrawal after stopping or changing opioids.
- Any sudden severe reaction after taking the medicine.
Warning: Respiratory depression is a major risk of opioid excess. Do not ignore breathing problems while using TarginAct®.
Storage and disposal
Store TarginAct® at or below 25 °C.
Do not remove the tablets from the outer carton until you need to use them. This helps protect the medicine.
Keep TarginAct® out of reach of children.
Expiry guidance is not specified in the source. Do not use medicine after the expiry date shown on the packaging, and ask your pharmacist how to dispose of unused medicine safely.
What the medicine contains
Active ingredients
Each prolonged-release tablet contains oxycodone hydrochloride and naloxone hydrochloride in one of the following strengths:
| Strength | Oxycodone hydrochloride | Naloxone hydrochloride | Lactose content |
|---|---|---|---|
| TarginAct® 5 mg/2,5 mg | 5 mg | 2,5 mg | 71,75 mg |
| TarginAct® 10 mg/5 mg | 10 mg | 5 mg | 64,25 mg |
| TarginAct® 20 mg/10 mg | 20 mg | 10 mg | 54,50 mg |
| TarginAct® 40 mg/20 mg | 40 mg | 20 mg | 109 mg |
Other ingredients
The tablet core contains:
- Ethylcellulose.
- Lactose monohydrate.
- Magnesium stearate.
- Stearyl alcohol.
- Talc.
TarginAct® 5 mg/2,5 mg also contains:
- Hydroxypropylcellulose.
TarginAct® 10 mg/5 mg, 20 mg/10 mg and 40 mg/20 mg also contain:
- Povidone K30.
The tablet coating contains:
- Polyvinyl alcohol.
- Macrogol.
- Talc.
- Titanium dioxide.
Colour ingredients differ by strength:
- TarginAct® 5 mg/2,5 mg contains Brilliant Blue FCF aluminium lake.
- TarginAct® 10 mg/5 mg contains no additional colourant.
- TarginAct® 20 mg/10 mg contains iron oxide red.
- TarginAct® 40 mg/20 mg contains iron oxide yellow.
Note: TarginAct® contains lactose. Do not use it if you have rare hereditary problems of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption.
Pack information and appearance
TarginAct® tablets are capsule-shaped prolonged-release tablets.
- TarginAct® 5 mg/2,5 mg: blue tablet, marked “OXN” on one side and “5” on the other.
- TarginAct® 10 mg/5 mg: white tablet, marked “OXN” on one side and “10” on the other.
- TarginAct® 20 mg/10 mg: pink tablet, marked “OXN” on one side and “20” on the other.
- TarginAct® 40 mg/20 mg: yellow tablet, marked “OXN” on one side and “40” on the other.
TarginAct® is supplied in clear PVC and silver aluminium foil blister packs of 28 tablets, packed in a cardboard carton.
South African registration numbers listed in the source are:
- TarginAct® 5 mg/2,5 mg: 46/2.9/0645
- TarginAct® 10 mg/5 mg: 46/2.9/0646
- TarginAct® 20 mg/10 mg: 46/2.9/0647
- TarginAct® 40 mg/20 mg: 46/2.9/0648
The holder of the certificate of registration is Mundipharma (Pty) Ltd, South Africa.
Practical FAQs
Can I take TarginAct® with food?
Yes. TarginAct® may be taken with or without food. Swallow it with enough liquid.
Can I break the tablet if it is hard to swallow?
No. Do not break, chew or crush TarginAct® tablets. They must be swallowed whole to keep the prolonged-release action working safely.
Why does TarginAct® contain naloxone?
Naloxone is included to help reduce the risk of constipation caused by opioid treatment. The oxycodone part helps with severe pain.
Can I use TarginAct® for sudden breakthrough pain?
TarginAct® is not intended for breakthrough pain because it releases medicine slowly. Your doctor may prescribe an immediate-release pain medicine as rescue treatment if needed.
What should I do if I need rescue pain medicine often?
The source states that needing more than two rescue doses per day usually suggests the TarginAct® dose may need upward adjustment. Speak to your doctor. Do not adjust the dose yourself.
Can I drink alcohol while taking TarginAct®?
The source warns that alcohol can increase central nervous system depressant effects when taken with TarginAct®. This may increase risks such as breathing depression. Ask your doctor for advice, especially before driving or using machinery.
Can I drive while taking TarginAct®?
TarginAct® may impair your ability to drive or use machines, especially when starting treatment, after a dose increase, when changing medicines, or when used with alcohol or other central nervous system depressants. Ask your medical practitioner whether driving is safe for you.
Is TarginAct® safe during pregnancy?
TarginAct® is not recommended during pregnancy or labour. Long-term oxycodone use during pregnancy may cause withdrawal symptoms in a newborn, and use during childbirth may cause breathing depression in the baby.
Can I breastfeed while taking TarginAct®?
No. Oxycodone passes into breast milk, and it is not known whether naloxone passes into breast milk. TarginAct® should not be used by mothers breastfeeding their infants.
Why might I see something like a tablet in my stool?
The empty prolonged-release tablet matrix may be visible in the stool. This is mentioned in the source.
Plain-language summary
TarginAct® is a strong Schedule 6 pain medicine for severe pain that needs an opioid. It contains oxycodone for pain relief and naloxone to help reduce the risk of constipation. Take it exactly as prescribed, usually twice a day, and swallow each tablet whole with enough liquid.
The most important safety rule is never to break, chew or crush the tablets. Get urgent medical help if you have slow or difficult breathing, extreme sleepiness, collapse, signs of overdose, a serious allergic reaction or convulsions. Speak to your doctor before stopping TarginAct®, because the dose may need to be reduced gradually.
