Lopinavir with ritonavir tablets
- Drugs List
- Therapeutic Indications
- Dosage
- Contraindications
- Precautions and Warnings
- Pregnancy and Lactation
- Side Effects
- Monograph
Presentation
Tablets of lopinavir containing ritonavir.
Drugs List
Therapeutic Indications
Uses
Antiretroviral combination therapy-HIV infected adults & children over 2yrs
Dosage
For adult and paediatric patients that may have difficulty swallowing, an oral solution of lopinavir with ritonavir is available. Refer to separate product information for dosage.
A once-daily dosing schedule may be considered in adult patients, where deemed clinically necessary for management of the patient. This dosing schedule may increase the risk of adverse reactions, and should not be used in patients with 3 or more protease inhibitor associated mutations.
The decision to treat protease inhibitor experienced HIV-1 infected patients with lopinavir and ritonavir should be based on individual viral resistance testing and treatment history of patients.
Adults
Standard dosing schedule
400mg/100mg twice daily.
Once-daily dosing schedule
800mg/200mg once daily.
Children
Children 2 years and above
Bodyweight of greater than 35kg (or BSA equal to or greater than 1.4 metres squared)
400mg/100mg twice daily.
Bodyweight of greater than 25kg, up to and including 35kg (or BSA equal to or greater than 0.9, and up to 1.4 metres squared)
300mg/75mg twice daily.
Bodyweight of greater than 15kg, up to and including 25kg (or BSA equal to or greater than 0.5, and up to 0.9 metres squared)
200mg/50mg twice daily.
Children 2 years and above, with concomitant efavirenz or nevirapine
BSA equal to or greater than 1.4 metres squared
500mg/125mg twice daily.
BSA equal to or greater than 1.2, and up to 1.4 metres squared
400mg/100mg twice daily.
BSA equal to or greater than 0.8, and up to 1.2 metres squared
300mg/75mg twice daily.
BSA equal to or greater than 0.5, and up to 0.8 metres squared
200mg/50mg twice daily.
Children under 2 years
Tablets are not recommended for use in children less than 2 years of age. An oral solution is available as an alternative.
Additional Dosage Information
Correct dosage of lopinavir with ritonavir should be achieved by the combined use of 100mg/25mg and 200mg/50mg tablets. Tablets should not be broken to achieve the correct dosage.
Contraindications
Acute porphyria
Breastfeeding
Long QT syndrome
Severe hepatic impairment
Torsade de pointes
Precautions and Warnings
Children under 2 years
Family history of long QT syndrome
Cardiac conduction defects
Electrolyte imbalance
Haemophilia
Hepatitis B
Hepatitis C
History of pancreatitis
History of torsade de pointes
Hypertriglyceridaemia
Mild hepatic impairment
Pregnancy
Structural cardiac disorder
Correct electrolyte disorders before treatment
Treatment does not prevent risk of transmission of HIV
Advise ability to drive/operate machinery may be affected by side effects
Monitor TSH when starting/stopping treatment if concurrent levothyroxine
Must be used in combination with other antiretrovirals
Treatment should be initiated by doctor experienced in HIV management
Autoimmune disorders can occur many months after initiation of treatment
Blood lipid and glucose levels may increase requiring treatment
Consider monitoring ECG in patients at risk of QT prolongation
Monitor serum amylase in patients at risk of pancreatitis
Monitor serum electrolytes
Monitor serum lipase in patients at risk of pancreatitis
Advise patient to report unexplained nausea,vomiting,abdominal pain
Advise patient to seek medical advice if joint aches or pain occur
Advise patient to seek medical advice if movement becomes difficult
Consider discontinuation if pancreatitis occurs
Inflammatory symptoms should be evaluated and treated appropriately
Risk of developing opportunistic infections
Discontinue if hepatic function deteriorates in pts with hepatic impairment
Advise patient not to take St John's wort concurrently
Female: Barrier or non-hormonal contraception advised during treatment
Advise haemophiliac patients of possibility of increased bleeding
Modest asymptomatic prolongation of the PR interval has been observed in some healthy adult subjects. Rare reports of 2nd or 3rd degree atrioventricular block in patients with underlying structural heart disease and pre-existing conduction system abnormalities or in patients also receiving drugs known to prolong the PR interval have been reported. Lopinavir with ritonavir should therefore be used with caution in such patients.
Blood lipid and glucose levels may increase during antiretroviral therapy. This may be linked to disease control and lifestyle. Refer to established HIV treatment guidelines for monitoring and manage lipid and glucose level disorders as appropriate.
Pregnancy and Lactation
Pregnancy
Use lopinavir with ritonavir with caution in pregnancy.
The manufacturer states that the prevalence of birth defects in newborns exposed to lopinavir with ritonavir in any trimester is comparable to the general population. They recommend that lopinavir with ritonavir can be used in pregnancy if clinically indicated. The once daily dosing schedule is not recommended due to lack of data.
Animal studies have shown reproductive toxicity, with Briggs (2015) suggesting a moderate risk in human pregnancy but concluding that the drug should not be withheld because of pregnancy if clinically necessary.
Lactation
Lopinavir with ritonavir is contraindicated in breastfeeding women. It is recommended that HIV infected women do not breast feed their infants in order to avoid transmission of HIV.
Use in breastfeeding is contraindicated by the manufacturer. It is not known whether this medicinal product is excreted in human milk; little data are available on the use of lopinavir in combination with ritonavir in breastfeeding. Animal studies suggest the drug is excreted in the milk.
The molecular weight of lopinavir and ritonavir combined, together with their lipid solubility, suggests that the drugs will be excreted in human breastmilk, but that high protein binding should limit this excretion (Briggs 2015).
Side Effects
Abdominal distension
Abdominal pain
Alopecia
Anaemia
Angioedema
Anxiety
Arteriosclerosis
Arthralgia
Asthenia
Atrioventricular block
Autoimmune hepatitis
Back pain
Cellulitis
Cerebrovascular accident
Cholangitis
Colitis
Constipation
Convulsions
Decrease in creatinine clearance
Deep vein thrombosis (DVT)
Dermatitis
Diabetes mellitus
Diarrhoea
Disturbances of appetite
Dizziness
Dream abnormalities
Dry mouth
Duodenitis
Dyspepsia
Eczema
Erectile dysfunction
Erythema multiforme
Faecal incontinence
Fatigue
Flatulence
Folliculitis
Furunculosis
Gastritis
Gastro-enteritis
Gastro-intestinal ulceration
Gastroesophageal reflux disease
Gastrointestinal bleeding
Graves' disease
Haematuria
Haemorrhoids
Headache
Hepatic steatosis
Hepatitis
Hepatomegaly
Hyperbilirubinaemia
Hypercholesterolaemia
Hyperglycaemia
Hyperlactataemia
Hypersensitivity reactions
Hypertension
Hypertriglyceridaemia
Hypogonadism
Immune Reactivation/Reconstitution Syndrome
Increase of liver transaminases
Insomnia
Insulin resistance
Jaundice
Leucopenia
Maculopapular rash
Menstrual disturbances
Migraine
Mouth ulcers
Muscle disorders
Muscle spasm
Muscle weakness
Musculoskeletal pain
Myalgia
Myocardial infarction
Nausea
Nephritis
Neuropathy
Neutropenia
Night sweats
Osteonecrosis
Pancreatitis
Prolongation of PR interval
Pruritus
Rash
Rectal haemorrhage
Reduced libido
Respiratory tract infection
Rhabdomyolysis
Skin infection
Stevens-Johnson syndrome
Stomatitis
Taste disturbances
Tinnitus
Tremor
Tricuspid valve incompetence
Urticaria
Vasculitis
Vertigo
Visual disturbances
Vomiting
Weight changes
Overdosage
It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).
Further Information
Last Full Review Date: April 2020
Reference Sources
Drugs in Pregnancy and Lactation: A Reference Guide to Fetal and Neonatal Risk, 10th edition (2015) ed. Briggs, G., Freeman, R. Wolters Kluwer Health, Philadelphia.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 11 April 2018
MHRA Drug Safety Update October 2018
Available at: https://www.mhra.gov.uk
Last accessed: 11/02/2019
Summary of Product Characteristics: Kaletra 100mg/25mg film-coated tablets. AbbVie Limited. Revised October 2019.
Summary of Product Characteristics: Kaletra 200mg/50mg film-coated tablets. AbbVie Limited. Revised March 2020.
Medscape UK | Univadis prescription drug monographs & interactions are based on FDB Multilex Content
FDB Disclaimer : FDB Multilex is intended for the use of healthcare professionals and is provided on the basis that the healthcare professionals will retain FULL and SOLE responsibility for deciding what treatment to prescribe or dispense for any particular patient or circumstance.