raltegravir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals | 2352 | 518048-05-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. The provirus is required to direct the production of progeny virus, so inhibiting integration prevents propagation of the viral infection.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 9 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 25.72 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 31.80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 24, 2008 | PMDA | Banyu Pharmaceutical Co., Ltd. | |
| Dec. 20, 2007 | EMA | ||
| Oct. 12, 2007 | FDA | MERCK SHARP DOHME |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Exposure during pregnancy | 1176.15 | 23.10 | 526 | 8738 | 120489 | 50475371 |
| Foetal exposure during pregnancy | 578.09 | 23.10 | 209 | 9055 | 27150 | 50568710 |
| Maternal exposure during pregnancy | 305.36 | 23.10 | 244 | 9020 | 159534 | 50436326 |
| Abortion spontaneous | 261.11 | 23.10 | 135 | 9129 | 41637 | 50554223 |
| Virologic failure | 245.20 | 23.10 | 57 | 9207 | 1507 | 50594353 |
| Premature baby | 226.39 | 23.10 | 95 | 9169 | 18242 | 50577618 |
| Immune reconstitution inflammatory syndrome | 190.37 | 23.10 | 61 | 9203 | 5455 | 50590405 |
| Blood HIV RNA increased | 141.11 | 23.10 | 30 | 9234 | 519 | 50595341 |
| Pathogen resistance | 140.88 | 23.10 | 49 | 9215 | 5640 | 50590220 |
| Lipodystrophy acquired | 139.22 | 23.10 | 35 | 9229 | 1294 | 50594566 |
| Drug reaction with eosinophilia and systemic symptoms | 130.58 | 23.10 | 75 | 9189 | 28349 | 50567511 |
| Premature delivery | 126.56 | 23.10 | 69 | 9195 | 23594 | 50572266 |
| Viral load increased | 123.67 | 23.10 | 31 | 9233 | 1132 | 50594728 |
| Viral mutation identified | 122.67 | 23.10 | 33 | 9231 | 1596 | 50594264 |
| Premature labour | 113.89 | 23.10 | 51 | 9213 | 11425 | 50584435 |
| Caesarean section | 113.53 | 23.10 | 56 | 9208 | 15583 | 50580277 |
| Spina bifida | 107.11 | 23.10 | 25 | 9239 | 672 | 50595188 |
| Ectopic kidney | 98.10 | 23.10 | 16 | 9248 | 54 | 50595806 |
| Abortion induced | 97.45 | 23.10 | 43 | 9221 | 9301 | 50586559 |
| Live birth | 88.14 | 23.10 | 48 | 9216 | 16360 | 50579500 |
| Foetal growth restriction | 87.33 | 23.10 | 36 | 9228 | 6591 | 50589269 |
| Treatment noncompliance | 86.46 | 23.10 | 59 | 9205 | 30091 | 50565769 |
| Sudden infant death syndrome | 86.45 | 23.10 | 17 | 9247 | 195 | 50595665 |
| Cloacal exstrophy | 84.60 | 23.10 | 16 | 9248 | 147 | 50595713 |
| Foetal death | 80.03 | 23.10 | 36 | 9228 | 8144 | 50587716 |
| Congenital genital malformation | 79.49 | 23.10 | 15 | 9249 | 136 | 50595724 |
| Bladder agenesis | 79.00 | 23.10 | 15 | 9249 | 141 | 50595719 |
| Drug resistance | 78.98 | 23.10 | 47 | 9217 | 18942 | 50576918 |
| Genitalia external ambiguous | 78.34 | 23.10 | 15 | 9249 | 148 | 50595712 |
| Caudal regression syndrome | 77.36 | 23.10 | 15 | 9249 | 159 | 50595701 |
| Meconium stain | 75.66 | 23.10 | 15 | 9249 | 180 | 50595680 |
| Gastrointestinal disorder congenital | 74.28 | 23.10 | 14 | 9250 | 126 | 50595734 |
| Tethered cord syndrome | 72.87 | 23.10 | 15 | 9249 | 220 | 50595640 |
| Anal atresia | 70.64 | 23.10 | 16 | 9248 | 375 | 50595485 |
| Meningomyelocele | 69.68 | 23.10 | 17 | 9247 | 554 | 50595306 |
| Congenital heart valve disorder | 68.68 | 23.10 | 12 | 9252 | 67 | 50595793 |
| Premature rupture of membranes | 67.62 | 23.10 | 27 | 9237 | 4553 | 50591307 |
| Neonatal respiratory arrest | 65.98 | 23.10 | 11 | 9253 | 44 | 50595816 |
| Gastrointestinal malformation | 64.40 | 23.10 | 13 | 9251 | 172 | 50595688 |
| Hepatocellular injury | 63.29 | 23.10 | 46 | 9218 | 25901 | 50569959 |
| Gastroschisis | 60.55 | 23.10 | 13 | 9251 | 236 | 50595624 |
| Exomphalos | 60.09 | 23.10 | 15 | 9249 | 538 | 50595322 |
| Congenital pulmonary valve disorder | 59.21 | 23.10 | 10 | 9254 | 44 | 50595816 |
| Umbilical cord abnormality | 58.80 | 23.10 | 15 | 9249 | 588 | 50595272 |
| Immune reconstitution inflammatory syndrome associated tuberculosis | 56.82 | 23.10 | 13 | 9251 | 319 | 50595541 |
| Hemivertebra | 56.61 | 23.10 | 11 | 9253 | 118 | 50595742 |
| Complication of delivery | 55.03 | 23.10 | 11 | 9253 | 138 | 50595722 |
| Congenital anomaly | 53.19 | 23.10 | 17 | 9247 | 1504 | 50594356 |
| Maternal drugs affecting foetus | 51.76 | 23.10 | 23 | 9241 | 5054 | 50590806 |
| Pulmonary valve sclerosis | 48.60 | 23.10 | 8 | 9256 | 29 | 50595831 |
| Pain | 48.21 | 23.10 | 23 | 9241 | 578880 | 50016980 |
| CD4 lymphocytes decreased | 46.97 | 23.10 | 15 | 9249 | 1324 | 50594536 |
| Neural tube defect | 46.55 | 23.10 | 10 | 9254 | 182 | 50595678 |
| Congenital choroid plexus cyst | 46.48 | 23.10 | 11 | 9253 | 314 | 50595546 |
| Generalised anxiety disorder | 46.29 | 23.10 | 16 | 9248 | 1804 | 50594056 |
| Congenital ectopic bladder | 46.20 | 23.10 | 9 | 9255 | 98 | 50595762 |
| Hyperbilirubinaemia | 45.92 | 23.10 | 26 | 9238 | 9544 | 50586316 |
| Cardiac murmur | 45.63 | 23.10 | 27 | 9237 | 10757 | 50585103 |
| Anencephaly | 45.47 | 23.10 | 10 | 9254 | 204 | 50595656 |
| Stillbirth | 45.23 | 23.10 | 22 | 9242 | 5930 | 50589930 |
| Drug interaction | 44.77 | 23.10 | 107 | 9157 | 199514 | 50396346 |
| Congenital hydrocephalus | 43.65 | 23.10 | 9 | 9255 | 133 | 50595727 |
| Drug ineffective | 43.43 | 23.10 | 52 | 9212 | 819281 | 49776579 |
| Genotype drug resistance test positive | 42.44 | 23.10 | 10 | 9254 | 280 | 50595580 |
| Cholestasis of pregnancy | 41.03 | 23.10 | 13 | 9251 | 1118 | 50594742 |
| Renal tubular dysfunction | 39.94 | 23.10 | 10 | 9254 | 363 | 50595497 |
| Low birth weight baby | 39.53 | 23.10 | 20 | 9244 | 5861 | 50589999 |
| Fall | 39.28 | 23.10 | 7 | 9257 | 334925 | 50260935 |
| Pre-eclampsia | 38.98 | 23.10 | 22 | 9242 | 8022 | 50587838 |
| Gestational diabetes | 37.76 | 23.10 | 21 | 9243 | 7444 | 50588416 |
| Mycoplasma genitalium infection | 37.32 | 23.10 | 6 | 9258 | 18 | 50595842 |
| Product size issue | 36.63 | 23.10 | 9 | 9255 | 302 | 50595558 |
| Viral load decreased | 35.79 | 23.10 | 6 | 9258 | 25 | 50595835 |
| Hepatitis fulminant | 34.85 | 23.10 | 15 | 9249 | 3053 | 50592807 |
| Hydrocephalus | 34.30 | 23.10 | 17 | 9247 | 4771 | 50591089 |
| Ventricular hypertrophy | 34.17 | 23.10 | 15 | 9249 | 3200 | 50592660 |
| Central obesity | 34.01 | 23.10 | 11 | 9253 | 1011 | 50594849 |
| Sepsis neonatal | 33.74 | 23.10 | 9 | 9255 | 421 | 50595439 |
| Oesophageal candidiasis | 33.62 | 23.10 | 17 | 9247 | 4977 | 50590883 |
| Large for dates baby | 32.85 | 23.10 | 9 | 9255 | 466 | 50595394 |
| Fatigue | 31.33 | 23.10 | 51 | 9213 | 707550 | 49888310 |
| Dyspnoea | 30.83 | 23.10 | 33 | 9231 | 547575 | 50048285 |
| Musculoskeletal deformity | 30.41 | 23.10 | 10 | 9254 | 968 | 50594892 |
| Eosinophilia | 30.22 | 23.10 | 26 | 9238 | 18626 | 50577234 |
| Mental disability | 29.54 | 23.10 | 6 | 9258 | 82 | 50595778 |
| Thymus hypoplasia | 29.42 | 23.10 | 5 | 9259 | 23 | 50595837 |
| CSF HIV escape syndrome | 28.77 | 23.10 | 6 | 9258 | 94 | 50595766 |
| Mitochondrial cytopathy | 28.69 | 23.10 | 7 | 9257 | 228 | 50595632 |
| Nephropathy toxic | 28.58 | 23.10 | 18 | 9246 | 8011 | 50587849 |
| Microcephaly | 28.04 | 23.10 | 9 | 9255 | 807 | 50595053 |
| Bacillus infection | 27.58 | 23.10 | 8 | 9256 | 510 | 50595350 |
| Bronchopulmonary dysplasia | 27.42 | 23.10 | 7 | 9257 | 275 | 50595585 |
| Diastasis recti abdominis | 27.40 | 23.10 | 5 | 9259 | 37 | 50595823 |
| Cholestasis | 26.95 | 23.10 | 28 | 9236 | 25373 | 50570487 |
| Small for dates baby | 26.76 | 23.10 | 13 | 9251 | 3492 | 50592368 |
| Antiviral drug level below therapeutic | 26.53 | 23.10 | 5 | 9259 | 45 | 50595815 |
| Hepatic cytolysis | 25.96 | 23.10 | 17 | 9247 | 8086 | 50587774 |
| Rash maculo-papular | 25.84 | 23.10 | 28 | 9236 | 26613 | 50569247 |
| Bacterial vulvovaginitis | 25.79 | 23.10 | 8 | 9256 | 642 | 50595218 |
| Chronic papillomatous dermatitis | 25.79 | 23.10 | 5 | 9259 | 53 | 50595807 |
| Patent ductus arteriosus | 25.70 | 23.10 | 13 | 9251 | 3807 | 50592053 |
| Arthralgia | 25.15 | 23.10 | 26 | 9238 | 438676 | 50157184 |
| Amniotic cavity infection | 24.91 | 23.10 | 9 | 9255 | 1154 | 50594706 |
| Dermatitis exfoliative | 24.74 | 23.10 | 14 | 9250 | 5128 | 50590732 |
| Abdominal discomfort | 24.74 | 23.10 | 6 | 9258 | 231635 | 50364225 |
| Heart disease congenital | 24.45 | 23.10 | 9 | 9255 | 1217 | 50594643 |
| Acute stress disorder | 24.09 | 23.10 | 6 | 9258 | 213 | 50595647 |
| Drug hypersensitivity | 24.04 | 23.10 | 8 | 9256 | 251002 | 50344858 |
| Hepatotoxicity | 23.63 | 23.10 | 27 | 9237 | 27199 | 50568661 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Depression | 834.75 | 14.35 | 563 | 17591 | 84584 | 29471789 |
| Drug interaction | 803.93 | 14.35 | 779 | 17375 | 196606 | 29359767 |
| Virologic failure | 449.74 | 14.35 | 134 | 18020 | 2713 | 29553660 |
| Lipodystrophy acquired | 375.66 | 14.35 | 119 | 18035 | 2975 | 29553398 |
| Immune reconstitution inflammatory syndrome | 348.01 | 14.35 | 143 | 18011 | 7659 | 29548714 |
| Foetal exposure during pregnancy | 316.18 | 14.35 | 218 | 17936 | 33649 | 29522724 |
| Pathogen resistance | 302.71 | 14.35 | 131 | 18023 | 7985 | 29548388 |
| Mitochondrial toxicity | 260.98 | 14.35 | 85 | 18069 | 2326 | 29554047 |
| Progressive external ophthalmoplegia | 247.69 | 14.35 | 71 | 18083 | 1246 | 29555127 |
| Viral mutation identified | 230.48 | 14.35 | 78 | 18076 | 2410 | 29553963 |
| Blood HIV RNA increased | 218.82 | 14.35 | 61 | 18093 | 963 | 29555410 |
| Eyelid ptosis | 210.82 | 14.35 | 89 | 18065 | 5097 | 29551276 |
| Loss of personal independence in daily activities | 200.94 | 14.35 | 148 | 18006 | 25292 | 29531081 |
| Viral load increased | 142.87 | 14.35 | 52 | 18102 | 1997 | 29554376 |
| Drug resistance | 140.79 | 14.35 | 112 | 18042 | 21428 | 29534945 |
| Psychiatric decompensation | 115.50 | 14.35 | 41 | 18113 | 1463 | 29554910 |
| Diplopia | 109.72 | 14.35 | 80 | 18074 | 13438 | 29542935 |
| Renal tubular disorder | 105.11 | 14.35 | 52 | 18102 | 4300 | 29552073 |
| CD4 lymphocytes decreased | 98.33 | 14.35 | 37 | 18117 | 1561 | 29554812 |
| Volvulus | 94.08 | 14.35 | 33 | 18121 | 1136 | 29555237 |
| Depression suicidal | 94.02 | 14.35 | 34 | 18120 | 1281 | 29555092 |
| Drug reaction with eosinophilia and systemic symptoms | 79.70 | 14.35 | 92 | 18062 | 27900 | 29528473 |
| Gene mutation | 78.50 | 14.35 | 28 | 18126 | 1013 | 29555360 |
| CSF HIV escape syndrome | 78.30 | 14.35 | 19 | 18135 | 167 | 29556206 |
| HIV-associated neurocognitive disorder | 77.39 | 14.35 | 21 | 18133 | 298 | 29556075 |
| Tearfulness | 76.35 | 14.35 | 31 | 18123 | 1605 | 29554768 |
| Brachydactyly | 71.82 | 14.35 | 18 | 18136 | 183 | 29556190 |
| Hepatitis C | 70.64 | 14.35 | 52 | 18102 | 8858 | 29547515 |
| Osteoporotic fracture | 68.52 | 14.35 | 25 | 18129 | 966 | 29555407 |
| Paranoia | 59.51 | 14.35 | 49 | 18105 | 9828 | 29546545 |
| Ophthalmoplegia | 58.93 | 14.35 | 26 | 18128 | 1656 | 29554717 |
| Depressive symptom | 55.23 | 14.35 | 25 | 18129 | 1692 | 29554681 |
| Hemivertebra | 55.11 | 14.35 | 13 | 18141 | 100 | 29556273 |
| Oesophageal atresia | 52.49 | 14.35 | 17 | 18137 | 456 | 29555917 |
| Genotype drug resistance test positive | 49.86 | 14.35 | 20 | 18134 | 1003 | 29555370 |
| Dyslipidaemia | 49.46 | 14.35 | 36 | 18118 | 6025 | 29550348 |
| Suicidal ideation | 48.57 | 14.35 | 81 | 18073 | 34635 | 29521738 |
| Cytomegalovirus chorioretinitis | 48.07 | 14.35 | 28 | 18126 | 3210 | 29553163 |
| Gastrointestinal tube insertion | 47.95 | 14.35 | 20 | 18134 | 1109 | 29555264 |
| Genital herpes | 45.77 | 14.35 | 16 | 18138 | 545 | 29555828 |
| Treatment failure | 43.63 | 14.35 | 80 | 18074 | 36859 | 29519514 |
| Osteoporosis | 42.30 | 14.35 | 42 | 18112 | 10727 | 29545646 |
| Drug level decreased | 41.89 | 14.35 | 33 | 18121 | 6214 | 29550159 |
| Oesophageal candidiasis | 41.33 | 14.35 | 27 | 18127 | 3794 | 29552579 |
| Renal impairment | 40.73 | 14.35 | 126 | 18028 | 81207 | 29475166 |
| Phalangeal hypoplasia | 38.77 | 14.35 | 9 | 18145 | 64 | 29556309 |
| Genital herpes simplex | 38.47 | 14.35 | 10 | 18144 | 119 | 29556254 |
| Anogenital dysplasia | 38.24 | 14.35 | 10 | 18144 | 122 | 29556251 |
| Premature baby | 38.18 | 14.35 | 50 | 18104 | 17230 | 29539143 |
| Laryngomalacia | 37.81 | 14.35 | 12 | 18142 | 301 | 29556072 |
| Anal cancer | 36.03 | 14.35 | 12 | 18142 | 352 | 29556021 |
| Dyspnoea | 35.64 | 14.35 | 94 | 18060 | 326638 | 29229735 |
| Blood creatine phosphokinase increased | 34.80 | 14.35 | 77 | 18077 | 40567 | 29515806 |
| Treatment noncompliance | 34.51 | 14.35 | 57 | 18097 | 24170 | 29532203 |
| Psychomotor skills impaired | 34.27 | 14.35 | 21 | 18133 | 2640 | 29553733 |
| Low birth weight baby | 34.10 | 14.35 | 30 | 18124 | 6578 | 29549795 |
| Completed suicide | 33.98 | 14.35 | 7 | 18147 | 90239 | 29466134 |
| Superior mesenteric artery syndrome | 33.00 | 14.35 | 8 | 18146 | 70 | 29556303 |
| Atrial fibrillation | 32.68 | 14.35 | 12 | 18142 | 105634 | 29450739 |
| Hypotension | 32.58 | 14.35 | 43 | 18111 | 194311 | 29362062 |
| Hepatic cirrhosis | 32.22 | 14.35 | 42 | 18112 | 14402 | 29541971 |
| Adverse event | 31.86 | 14.35 | 43 | 18111 | 15248 | 29541125 |
| Pneumonia | 31.32 | 14.35 | 97 | 18057 | 320075 | 29236298 |
| Drug abuse | 30.48 | 14.35 | 6 | 18148 | 79877 | 29476496 |
| Fanconi syndrome acquired | 30.21 | 14.35 | 17 | 18137 | 1825 | 29554548 |
| HIV lipodystrophy | 29.83 | 14.35 | 6 | 18148 | 19 | 29556354 |
| Congenital mitral valve incompetence | 29.78 | 14.35 | 8 | 18146 | 109 | 29556264 |
| Intestinal malrotation | 28.74 | 14.35 | 6 | 18148 | 24 | 29556349 |
| Congenital skin dimples | 26.68 | 14.35 | 8 | 18146 | 165 | 29556208 |
| HIV associated nephropathy | 26.25 | 14.35 | 9 | 18145 | 289 | 29556084 |
| Laryngectomy | 25.59 | 14.35 | 4 | 18150 | 0 | 29556373 |
| Dysphagia | 25.56 | 14.35 | 83 | 18071 | 54843 | 29501530 |
| Haemophilic arthropathy | 25.43 | 14.35 | 7 | 18147 | 105 | 29556268 |
| Syphilis | 24.93 | 14.35 | 9 | 18145 | 337 | 29556036 |
| Congenital vesicoureteric reflux | 24.59 | 14.35 | 5 | 18149 | 17 | 29556356 |
| Enanthema | 24.56 | 14.35 | 9 | 18145 | 352 | 29556021 |
| Strongyloidiasis | 24.19 | 14.35 | 16 | 18138 | 2296 | 29554077 |
| Fall | 24.16 | 14.35 | 45 | 18109 | 177133 | 29379240 |
| Hyperlipidaemia | 24.12 | 14.35 | 34 | 18120 | 12556 | 29543817 |
| Erosive duodenitis | 24.01 | 14.35 | 13 | 18141 | 1294 | 29555079 |
| Psychotic disorder | 23.92 | 14.35 | 44 | 18110 | 20310 | 29536063 |
| Osteonecrosis | 23.69 | 14.35 | 35 | 18119 | 13484 | 29542889 |
| Congenital foot malformation | 23.64 | 14.35 | 9 | 18145 | 392 | 29555981 |
| Nephropathy toxic | 23.56 | 14.35 | 31 | 18123 | 10725 | 29545648 |
| VACTERL syndrome | 23.35 | 14.35 | 4 | 18150 | 3 | 29556370 |
| Liver disorder | 23.10 | 14.35 | 52 | 18102 | 27697 | 29528676 |
| Cholestasis | 23.02 | 14.35 | 47 | 18107 | 23415 | 29532958 |
| Disease progression | 22.61 | 14.35 | 11 | 18143 | 81905 | 29474468 |
| Drug level increased | 22.56 | 14.35 | 41 | 18113 | 18746 | 29537627 |
| Hyperbilirubinaemia | 22.43 | 14.35 | 36 | 18118 | 14898 | 29541475 |
| HIV infection | 22.41 | 14.35 | 12 | 18142 | 1169 | 29555204 |
| Drug-induced liver injury | 21.99 | 14.35 | 44 | 18110 | 21611 | 29534762 |
| Antiviral drug level above therapeutic | 21.61 | 14.35 | 5 | 18149 | 35 | 29556338 |
| Acute hepatitis C | 21.44 | 14.35 | 6 | 18148 | 96 | 29556277 |
| Chronic hepatitis C | 21.27 | 14.35 | 8 | 18146 | 337 | 29556036 |
| Back pain | 21.13 | 14.35 | 19 | 18135 | 102265 | 29454108 |
| Lipohypertrophy | 20.84 | 14.35 | 7 | 18147 | 211 | 29556162 |
| Confusional state | 20.69 | 14.35 | 29 | 18125 | 127848 | 29428525 |
| Hemiparaesthesia | 20.60 | 14.35 | 5 | 18149 | 44 | 29556329 |
| Nephrolithiasis | 20.56 | 14.35 | 47 | 18107 | 25287 | 29531086 |
| Malignant neoplasm progression | 20.26 | 14.35 | 10 | 18144 | 73849 | 29482524 |
| Infection | 20.15 | 14.35 | 11 | 18143 | 76740 | 29479633 |
| Respiratory failure | 20.11 | 14.35 | 18 | 18136 | 97113 | 29459260 |
| Hepatic enzyme decreased | 20.02 | 14.35 | 5 | 18149 | 50 | 29556323 |
| Heart transplant rejection | 19.91 | 14.35 | 11 | 18143 | 1140 | 29555233 |
| Mycobacterium avium complex infection | 19.71 | 14.35 | 14 | 18140 | 2255 | 29554118 |
| Lymphoma | 19.51 | 14.35 | 27 | 18127 | 9801 | 29546572 |
| White matter lesion | 19.45 | 14.35 | 9 | 18145 | 641 | 29555732 |
| Glucose tolerance impaired | 19.25 | 14.35 | 15 | 18139 | 2779 | 29553594 |
| Hyperphagia | 19.14 | 14.35 | 11 | 18143 | 1229 | 29555144 |
| Jaundice | 19.14 | 14.35 | 50 | 18104 | 29246 | 29527127 |
| Acquired gene mutation | 19.00 | 14.35 | 11 | 18143 | 1247 | 29555126 |
| Atypical mycobacterial infection | 18.80 | 14.35 | 9 | 18145 | 692 | 29555681 |
| Congenital renal disorder | 18.69 | 14.35 | 5 | 18149 | 67 | 29556306 |
| Hypertriglyceridaemia | 18.67 | 14.35 | 23 | 18131 | 7452 | 29548921 |
| Choroiditis | 18.64 | 14.35 | 10 | 18144 | 978 | 29555395 |
| Hepatitis cholestatic | 18.51 | 14.35 | 22 | 18132 | 6871 | 29549502 |
| Drug ineffective | 18.46 | 14.35 | 139 | 18015 | 363031 | 29193342 |
| Constipation | 18.35 | 14.35 | 26 | 18128 | 114134 | 29442239 |
| Meningomyelocele | 18.28 | 14.35 | 6 | 18148 | 168 | 29556205 |
| Drug hypersensitivity | 17.67 | 14.35 | 10 | 18144 | 68396 | 29487977 |
| Nephrocalcinosis | 17.65 | 14.35 | 8 | 18146 | 543 | 29555830 |
| Febrile neutropenia | 17.61 | 14.35 | 26 | 18128 | 112214 | 29444159 |
| Cardiac arrest | 17.55 | 14.35 | 16 | 18138 | 85575 | 29470798 |
| Prescribed overdose | 17.45 | 14.35 | 24 | 18130 | 8659 | 29547714 |
| Infusion related reaction | 17.37 | 14.35 | 3 | 18151 | 43883 | 29512490 |
| Hepatitis | 17.36 | 14.35 | 39 | 18115 | 20744 | 29535629 |
| Cerebral ventricle dilatation | 17.15 | 14.35 | 9 | 18145 | 841 | 29555532 |
| Vertigo | 17.13 | 14.35 | 40 | 18114 | 21821 | 29534552 |
| Glycosuria | 17.12 | 14.35 | 10 | 18144 | 1152 | 29555221 |
| Congenital syphilis | 17.11 | 14.35 | 3 | 18151 | 3 | 29556370 |
| Tracheal fistula repair | 17.11 | 14.35 | 3 | 18151 | 3 | 29556370 |
| Cardiomyopathy acute | 17.04 | 14.35 | 4 | 18150 | 30 | 29556343 |
| Lymphocytic infiltration | 16.93 | 14.35 | 8 | 18146 | 597 | 29555776 |
| Maternal drugs affecting foetus | 16.82 | 14.35 | 16 | 18138 | 3877 | 29552496 |
| Myelocytosis | 16.82 | 14.35 | 4 | 18150 | 32 | 29556341 |
| Abnormal dreams | 16.82 | 14.35 | 21 | 18133 | 6899 | 29549474 |
| Congenital cystic kidney disease | 16.75 | 14.35 | 7 | 18147 | 390 | 29555983 |
| Myopathy | 16.66 | 14.35 | 26 | 18128 | 10507 | 29545866 |
| Toxicity to various agents | 16.64 | 14.35 | 53 | 18101 | 173608 | 29382765 |
| Retinal toxicity | 16.63 | 14.35 | 7 | 18147 | 397 | 29555976 |
| Renal failure | 16.55 | 14.35 | 127 | 18027 | 118472 | 29437901 |
| Immune reconstitution inflammatory syndrome associated tuberculosis | 16.52 | 14.35 | 7 | 18147 | 404 | 29555969 |
| Oesophageal carcinoma | 16.51 | 14.35 | 17 | 18137 | 4530 | 29551843 |
| Intensive care unit acquired weakness | 16.28 | 14.35 | 9 | 18145 | 934 | 29555439 |
| Blood pressure increased | 16.10 | 14.35 | 13 | 18141 | 73790 | 29482583 |
| Hepatic failure | 15.91 | 14.35 | 49 | 18105 | 31463 | 29524910 |
| Oxygen saturation decreased | 15.88 | 14.35 | 4 | 18150 | 44933 | 29511440 |
| Congenital hydronephrosis | 15.79 | 14.35 | 8 | 18146 | 695 | 29555678 |
| Kidney enlargement | 15.75 | 14.35 | 8 | 18146 | 699 | 29555674 |
| Birth trauma | 15.58 | 14.35 | 3 | 18151 | 7 | 29556366 |
| Pulmonary tuberculosis | 15.43 | 14.35 | 16 | 18138 | 4299 | 29552074 |
| Pancreatitis acute | 15.30 | 14.35 | 41 | 18113 | 24344 | 29532029 |
| Retinitis pigmentosa | 15.28 | 14.35 | 4 | 18150 | 49 | 29556324 |
| Pain | 15.28 | 14.35 | 54 | 18100 | 171378 | 29384995 |
| Cardio-respiratory arrest | 15.21 | 14.35 | 6 | 18148 | 50595 | 29505778 |
| Renal disorder | 15.21 | 14.35 | 39 | 18115 | 22556 | 29533817 |
| Subacute combined cord degeneration | 15.10 | 14.35 | 5 | 18149 | 144 | 29556229 |
| Hepatorenal syndrome | 15.07 | 14.35 | 12 | 18142 | 2294 | 29554079 |
| Seborrhoeic dermatitis | 15.06 | 14.35 | 10 | 18144 | 1443 | 29554930 |
| Tracheal deviation | 15.04 | 14.35 | 3 | 18151 | 9 | 29556364 |
| Liver transplant | 15.02 | 14.35 | 12 | 18142 | 2304 | 29554069 |
| Cachexia | 15.00 | 14.35 | 19 | 18135 | 6330 | 29550043 |
| Dermatitis exfoliative | 14.82 | 14.35 | 19 | 18135 | 6406 | 29549967 |
| Adrenal suppression | 14.78 | 14.35 | 7 | 18147 | 525 | 29555848 |
| Sepsis | 14.77 | 14.35 | 42 | 18112 | 142640 | 29413733 |
| Congenital ureteric anomaly | 14.72 | 14.35 | 4 | 18150 | 57 | 29556316 |
| Adrenogenital syndrome | 14.66 | 14.35 | 4 | 18150 | 58 | 29556315 |
| Hepatocellular injury | 14.64 | 14.35 | 37 | 18117 | 21206 | 29535167 |
| Chest discomfort | 14.59 | 14.35 | 5 | 18149 | 45978 | 29510395 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Virologic failure | 876.88 | 14.60 | 208 | 21029 | 3258 | 64474237 |
| Drug interaction | 719.11 | 14.60 | 729 | 20508 | 361354 | 64116141 |
| Depression | 552.84 | 14.60 | 467 | 20770 | 182824 | 64294671 |
| Pathogen resistance | 542.41 | 14.60 | 190 | 21047 | 12353 | 64465142 |
| Viral mutation identified | 486.91 | 14.60 | 129 | 21108 | 3217 | 64474278 |
| Immune reconstitution inflammatory syndrome | 478.95 | 14.60 | 173 | 21064 | 12297 | 64465198 |
| Lipodystrophy acquired | 477.02 | 14.60 | 132 | 21105 | 3895 | 64473600 |
| Blood HIV RNA increased | 464.99 | 14.60 | 106 | 21131 | 1378 | 64476117 |
| Mitochondrial toxicity | 303.50 | 14.60 | 85 | 21152 | 2621 | 64474874 |
| Progressive external ophthalmoplegia | 296.09 | 14.60 | 72 | 21165 | 1255 | 64476240 |
| Exposure during pregnancy | 250.11 | 14.60 | 206 | 21031 | 77469 | 64400026 |
| Viral load increased | 237.87 | 14.60 | 69 | 21168 | 2418 | 64475077 |
| Drug resistance | 216.16 | 14.60 | 138 | 21099 | 34964 | 64442531 |
| Eyelid ptosis | 202.07 | 14.60 | 86 | 21151 | 9439 | 64468056 |
| Abortion spontaneous | 201.43 | 14.60 | 117 | 21120 | 25026 | 64452469 |
| Maternal exposure during pregnancy | 195.92 | 14.60 | 197 | 21040 | 95687 | 64381808 |
| Drug reaction with eosinophilia and systemic symptoms | 185.41 | 14.60 | 149 | 21088 | 54068 | 64423427 |
| Loss of personal independence in daily activities | 142.70 | 14.60 | 146 | 21091 | 72308 | 64405187 |
| Psychiatric decompensation | 128.59 | 14.60 | 43 | 21194 | 2420 | 64475075 |
| Foetal exposure during pregnancy | 117.25 | 14.60 | 47 | 21190 | 4429 | 64473066 |
| Diplopia | 112.08 | 14.60 | 83 | 21154 | 26682 | 64450813 |
| CSF HIV escape syndrome | 111.46 | 14.60 | 25 | 21212 | 300 | 64477195 |
| Renal tubular disorder | 107.26 | 14.60 | 48 | 21189 | 5939 | 64471556 |
| CD4 lymphocytes decreased | 105.61 | 14.60 | 37 | 21200 | 2398 | 64475097 |
| Gene mutation | 99.45 | 14.60 | 34 | 21203 | 2048 | 64475447 |
| Depression suicidal | 93.70 | 14.60 | 34 | 21203 | 2441 | 64475054 |
| Treatment noncompliance | 86.24 | 14.60 | 88 | 21149 | 43394 | 64434101 |
| HIV-associated neurocognitive disorder | 84.67 | 14.60 | 20 | 21217 | 306 | 64477189 |
| Premature labour | 84.58 | 14.60 | 44 | 21193 | 7576 | 64469919 |
| Hepatitis C | 82.25 | 14.60 | 49 | 21188 | 10966 | 64466529 |
| Premature delivery | 78.61 | 14.60 | 58 | 21179 | 18531 | 64458964 |
| Abortion induced | 71.23 | 14.60 | 37 | 21200 | 6351 | 64471144 |
| Genotype drug resistance test positive | 69.85 | 14.60 | 22 | 21215 | 1022 | 64476473 |
| Tearfulness | 69.73 | 14.60 | 33 | 21204 | 4640 | 64472855 |
| Hyperbilirubinaemia | 69.73 | 14.60 | 57 | 21180 | 21148 | 64456347 |
| Renal impairment | 66.43 | 14.60 | 141 | 21096 | 134876 | 64342619 |
| Paranoia | 64.64 | 14.60 | 49 | 21188 | 16303 | 64461192 |
| Immune reconstitution inflammatory syndrome associated tuberculosis | 63.21 | 14.60 | 19 | 21218 | 754 | 64476741 |
| Caesarean section | 61.23 | 14.60 | 41 | 21196 | 11233 | 64466262 |
| Nephropathy toxic | 59.53 | 14.60 | 48 | 21189 | 17466 | 64460029 |
| Ophthalmoplegia | 59.30 | 14.60 | 25 | 21212 | 2677 | 64474818 |
| Live birth | 59.06 | 14.60 | 40 | 21197 | 11164 | 64466331 |
| Oesophageal candidiasis | 58.13 | 14.60 | 35 | 21202 | 7982 | 64469513 |
| Depressive symptom | 55.82 | 14.60 | 28 | 21209 | 4468 | 64473027 |
| Osteoporotic fracture | 55.50 | 14.60 | 26 | 21211 | 3572 | 64473923 |
| Premature baby | 54.70 | 14.60 | 25 | 21212 | 3247 | 64474248 |
| Foetal death | 53.93 | 14.60 | 30 | 21207 | 5900 | 64471595 |
| Dyslipidaemia | 53.55 | 14.60 | 35 | 21202 | 9207 | 64468288 |
| Genital herpes | 53.47 | 14.60 | 21 | 21216 | 1874 | 64475621 |
| Pain | 51.61 | 14.60 | 64 | 21173 | 553447 | 63924048 |
| Premature rupture of membranes | 51.49 | 14.60 | 25 | 21212 | 3719 | 64473776 |
| Hepatocellular injury | 50.22 | 14.60 | 68 | 21169 | 45167 | 64432328 |
| Completed suicide | 48.21 | 14.60 | 8 | 21229 | 224406 | 64253089 |
| Cytomegalovirus chorioretinitis | 47.84 | 14.60 | 26 | 21211 | 4886 | 64472609 |
| Renal failure | 46.07 | 14.60 | 148 | 21089 | 181540 | 64295955 |
| Psychomotor skills impaired | 44.97 | 14.60 | 23 | 21214 | 3822 | 64473673 |
| Fall | 44.55 | 14.60 | 43 | 21194 | 416783 | 64060712 |
| Drug-induced liver injury | 43.15 | 14.60 | 65 | 21172 | 47578 | 64429917 |
| Hepatic cirrhosis | 42.90 | 14.60 | 48 | 21189 | 26250 | 64451245 |
| Dyspnoea | 42.75 | 14.60 | 110 | 21127 | 718564 | 63758931 |
| Fanconi syndrome acquired | 42.06 | 14.60 | 19 | 21218 | 2402 | 64475093 |
| Peripheral swelling | 41.64 | 14.60 | 9 | 21228 | 209144 | 64268351 |
| Drug hypersensitivity | 40.30 | 14.60 | 14 | 21223 | 237801 | 64239694 |
| Syphilis | 40.17 | 14.60 | 12 | 21225 | 466 | 64477029 |
| Generalised anxiety disorder | 39.64 | 14.60 | 17 | 21220 | 1898 | 64475597 |
| Joint swelling | 39.50 | 14.60 | 11 | 21226 | 215371 | 64262124 |
| Cholestasis | 38.91 | 14.60 | 60 | 21177 | 44812 | 64432683 |
| Pulmonary tuberculosis | 38.51 | 14.60 | 26 | 21211 | 7218 | 64470277 |
| Mitochondrial cytopathy | 38.00 | 14.60 | 11 | 21226 | 382 | 64477113 |
| Stillbirth | 37.54 | 14.60 | 20 | 21217 | 3613 | 64473882 |
| Dermatitis exfoliative | 36.51 | 14.60 | 29 | 21208 | 10323 | 64467172 |
| Genital herpes simplex | 35.92 | 14.60 | 10 | 21227 | 301 | 64477194 |
| Suicidal ideation | 35.63 | 14.60 | 72 | 21165 | 66470 | 64411025 |
| Cachexia | 35.06 | 14.60 | 27 | 21210 | 9190 | 64468305 |
| HIV lipodystrophy | 34.60 | 14.60 | 6 | 21231 | 15 | 64477480 |
| Spina bifida | 34.00 | 14.60 | 7 | 21230 | 54 | 64477441 |
| Mycoplasma genitalium infection | 33.80 | 14.60 | 6 | 21231 | 18 | 64477477 |
| Blood creatine phosphokinase increased | 33.32 | 14.60 | 65 | 21172 | 58493 | 64419002 |
| Liver transplant | 32.63 | 14.60 | 19 | 21218 | 4073 | 64473422 |
| Strongyloidiasis | 31.89 | 14.60 | 17 | 21220 | 3073 | 64474422 |
| Superior mesenteric artery syndrome | 31.80 | 14.60 | 8 | 21229 | 161 | 64477334 |
| Renal tubular dysfunction | 31.75 | 14.60 | 11 | 21226 | 689 | 64476806 |
| HIV associated nephropathy | 31.68 | 14.60 | 9 | 21228 | 292 | 64477203 |
| Enanthema | 31.14 | 14.60 | 11 | 21226 | 730 | 64476765 |
| Psychotic disorder | 31.05 | 14.60 | 47 | 21190 | 34531 | 64442964 |
| Atrial fibrillation | 30.88 | 14.60 | 9 | 21228 | 171080 | 64306415 |
| Cushingoid | 30.52 | 14.60 | 23 | 21214 | 7580 | 64469915 |
| Central obesity | 30.39 | 14.60 | 13 | 21224 | 1442 | 64476053 |
| Anogenital dysplasia | 29.95 | 14.60 | 7 | 21230 | 102 | 64477393 |
| Infection | 29.44 | 14.60 | 12 | 21225 | 184868 | 64292627 |
| Drug ineffective | 29.37 | 14.60 | 160 | 21077 | 840087 | 63637408 |
| Abdominal discomfort | 28.77 | 14.60 | 12 | 21225 | 182310 | 64295185 |
| Erosive duodenitis | 28.61 | 14.60 | 13 | 21224 | 1665 | 64475830 |
| Hepatitis cholestatic | 28.56 | 14.60 | 27 | 21210 | 12128 | 64465367 |
| White matter lesion | 28.29 | 14.60 | 13 | 21224 | 1709 | 64475786 |
| Adrenal suppression | 28.20 | 14.60 | 12 | 21225 | 1315 | 64476180 |
| Nephrolithiasis | 27.97 | 14.60 | 51 | 21186 | 43632 | 64433863 |
| Jaundice | 27.78 | 14.60 | 54 | 21183 | 48458 | 64429037 |
| Rash maculo-papular | 27.73 | 14.60 | 53 | 21184 | 46973 | 64430522 |
| Pancreatitis acute | 27.40 | 14.60 | 50 | 21187 | 42805 | 64434690 |
| Hepatic failure | 27.38 | 14.60 | 58 | 21179 | 55336 | 64422159 |
| Hepatic cytolysis | 27.05 | 14.60 | 28 | 21209 | 14021 | 64463474 |
| Proteinuria | 26.79 | 14.60 | 39 | 21198 | 27684 | 64449811 |
| Back pain | 26.47 | 14.60 | 26 | 21211 | 250145 | 64227350 |
| Injection site pain | 26.20 | 14.60 | 3 | 21234 | 111405 | 64366090 |
| Drug intolerance | 25.69 | 14.60 | 15 | 21222 | 187977 | 64289518 |
| Mycobacterium avium complex infection | 25.50 | 14.60 | 16 | 21221 | 3924 | 64473571 |
| Pancytopenia | 25.45 | 14.60 | 104 | 21133 | 143205 | 64334290 |
| Hepatic encephalopathy | 25.42 | 14.60 | 33 | 21204 | 21033 | 64456462 |
| Hepatitis fulminant | 25.23 | 14.60 | 19 | 21218 | 6255 | 64471240 |
| Cholestasis of pregnancy | 25.22 | 14.60 | 10 | 21227 | 915 | 64476580 |
| Anal cancer | 25.07 | 14.60 | 9 | 21228 | 626 | 64476869 |
| Acute hepatitis C | 25.07 | 14.60 | 7 | 21230 | 213 | 64477282 |
| Acute stress disorder | 24.93 | 14.60 | 8 | 21229 | 395 | 64477100 |
| Retinal toxicity | 24.90 | 14.60 | 11 | 21226 | 1319 | 64476176 |
| Nephrocalcinosis | 24.87 | 14.60 | 11 | 21226 | 1323 | 64476172 |
| HIV infection | 24.64 | 14.60 | 10 | 21227 | 972 | 64476523 |
| Confusional state | 24.47 | 14.60 | 30 | 21207 | 261114 | 64216381 |
| Antiviral drug level below therapeutic | 24.12 | 14.60 | 5 | 21232 | 40 | 64477455 |
| Haemolytic anaemia | 23.98 | 14.60 | 28 | 21209 | 16025 | 64461470 |
| Choroiditis | 23.66 | 14.60 | 10 | 21227 | 1077 | 64476418 |
| Hepatotoxicity | 23.52 | 14.60 | 45 | 21192 | 39917 | 64437578 |
| Pain in extremity | 23.31 | 14.60 | 40 | 21197 | 303045 | 64174450 |
| Pre-eclampsia | 23.15 | 14.60 | 18 | 21219 | 6213 | 64471282 |
| Chest discomfort | 23.09 | 14.60 | 5 | 21232 | 116101 | 64361394 |
| Brachydactyly | 23.07 | 14.60 | 4 | 21233 | 10 | 64477485 |
| Aspartate aminotransferase increased | 22.93 | 14.60 | 89 | 21148 | 119699 | 64357796 |
| Hypotension | 22.81 | 14.60 | 58 | 21179 | 380916 | 64096579 |
| Oesophageal carcinoma | 22.80 | 14.60 | 16 | 21221 | 4727 | 64472768 |
| Contraindicated product administered | 22.79 | 14.60 | 4 | 21233 | 107825 | 64369670 |
| Hypertriglyceridaemia | 22.79 | 14.60 | 23 | 21214 | 11182 | 64466313 |
| Face oedema | 22.72 | 14.60 | 34 | 21203 | 24727 | 64452768 |
| Oxygen saturation decreased | 22.60 | 14.60 | 4 | 21233 | 107172 | 64370323 |
| Eosinophilia | 22.56 | 14.60 | 43 | 21194 | 38033 | 64439462 |
| Multiple-drug resistance | 22.47 | 14.60 | 18 | 21219 | 6484 | 64471011 |
| Sinusitis | 22.39 | 14.60 | 10 | 21227 | 145918 | 64331577 |
| Nasopharyngitis | 22.37 | 14.60 | 19 | 21218 | 196054 | 64281441 |
| Drug level decreased | 22.28 | 14.60 | 23 | 21214 | 11480 | 64466015 |
| Abortion spontaneous incomplete | 21.85 | 14.60 | 4 | 21233 | 15 | 64477480 |
| Dysphagia | 21.80 | 14.60 | 81 | 21156 | 106731 | 64370764 |
| Product size issue | 21.73 | 14.60 | 8 | 21229 | 598 | 64476897 |
| Treatment failure | 21.72 | 14.60 | 86 | 21151 | 116730 | 64360765 |
| Hepatitis B | 21.71 | 14.60 | 19 | 21218 | 7726 | 64469769 |
| Tuberculosis | 21.61 | 14.60 | 24 | 21213 | 13014 | 64464481 |
| Therapeutic product effect decreased | 20.93 | 14.60 | 6 | 21231 | 115345 | 64362150 |
| Acquired gene mutation | 20.71 | 14.60 | 11 | 21226 | 1975 | 64475520 |
| Mycobacterium avium complex immune restoration disease | 20.60 | 14.60 | 4 | 21233 | 22 | 64477473 |
| Blood pressure increased | 20.58 | 14.60 | 16 | 21221 | 172536 | 64304959 |
| Hepatitis | 20.55 | 14.60 | 46 | 21191 | 45536 | 64431959 |
| Contusion | 20.55 | 14.60 | 6 | 21231 | 113959 | 64363536 |
| Viral load decreased | 20.30 | 14.60 | 4 | 21233 | 24 | 64477471 |
| Hepatic enzyme decreased | 20.15 | 14.60 | 5 | 21232 | 95 | 64477400 |
| Pneumocystis jirovecii pneumonia | 19.93 | 14.60 | 34 | 21203 | 27600 | 64449895 |
| Bacterial vulvovaginitis | 19.82 | 14.60 | 7 | 21230 | 464 | 64477031 |
| Lipohypertrophy | 19.65 | 14.60 | 8 | 21229 | 784 | 64476711 |
| Alanine aminotransferase increased | 19.47 | 14.60 | 94 | 21143 | 138937 | 64338558 |
| Psychomotor retardation | 19.42 | 14.60 | 15 | 21222 | 5128 | 64472367 |
| Pneumonia | 19.24 | 14.60 | 107 | 21130 | 559469 | 63918026 |
| Gastroschisis | 18.98 | 14.60 | 3 | 21234 | 3 | 64477492 |
| Renal colic | 18.97 | 14.60 | 11 | 21226 | 2341 | 64475154 |
| Hemiparaesthesia | 18.96 | 14.60 | 5 | 21232 | 122 | 64477373 |
| Lower respiratory tract infection | 18.96 | 14.60 | 4 | 21233 | 94610 | 64382885 |
| Chronic hepatitis C | 18.85 | 14.60 | 7 | 21230 | 536 | 64476959 |
| Osteoporosis | 18.45 | 14.60 | 42 | 21195 | 42038 | 64435457 |
| Toxic skin eruption | 18.44 | 14.60 | 27 | 21210 | 19257 | 64458238 |
| Chronic kidney disease | 18.26 | 14.60 | 51 | 21186 | 57868 | 64419627 |
| Stevens-Johnson syndrome | 18.25 | 14.60 | 37 | 21200 | 34212 | 64443283 |
| Constipation | 17.87 | 14.60 | 30 | 21207 | 229307 | 64248188 |
| Polyhydramnios | 17.69 | 14.60 | 9 | 21228 | 1478 | 64476017 |
| Therapeutic product effect incomplete | 17.67 | 14.60 | 6 | 21231 | 103476 | 64374019 |
| Lymphadenopathy | 17.66 | 14.60 | 44 | 21193 | 46642 | 64430853 |
| Glycosuria | 17.53 | 14.60 | 10 | 21227 | 2064 | 64475431 |
| Sudden infant death syndrome | 17.49 | 14.60 | 5 | 21232 | 166 | 64477329 |
| Prescribed overdose | 17.36 | 14.60 | 27 | 21210 | 20304 | 64457191 |
| Blood creatinine increased | 17.03 | 14.60 | 89 | 21148 | 135693 | 64341802 |
| Anaemia | 17.01 | 14.60 | 195 | 21042 | 378485 | 64099010 |
| Plasmablastic lymphoma | 16.92 | 14.60 | 6 | 21231 | 403 | 64477092 |
| Osteonecrosis | 16.87 | 14.60 | 32 | 21205 | 28197 | 64449298 |
| Bacillus infection | 16.70 | 14.60 | 7 | 21230 | 739 | 64476756 |
| Alopecia | 16.63 | 14.60 | 18 | 21219 | 165672 | 64311823 |
| Musculoskeletal stiffness | 16.59 | 14.60 | 10 | 21227 | 123196 | 64354299 |
| Intensive care unit acquired weakness | 16.43 | 14.60 | 9 | 21228 | 1718 | 64475777 |
| Lactic acidosis | 16.43 | 14.60 | 51 | 21186 | 61359 | 64416136 |
| Foetal growth restriction | 16.41 | 14.60 | 9 | 21228 | 1721 | 64475774 |
| Heart rate increased | 16.37 | 14.60 | 6 | 21231 | 98669 | 64378826 |
| Loss of consciousness | 16.17 | 14.60 | 15 | 21222 | 148350 | 64329145 |
| Seborrhoeic dermatitis | 15.96 | 14.60 | 9 | 21228 | 1817 | 64475678 |
| Urticaria | 15.93 | 14.60 | 15 | 21222 | 147302 | 64330193 |
| HIV viraemia | 15.93 | 14.60 | 4 | 21233 | 80 | 64477415 |
| Hepatic function abnormal | 15.91 | 14.60 | 52 | 21185 | 64261 | 64413234 |
| Atypical mycobacterial infection | 15.81 | 14.60 | 8 | 21229 | 1300 | 64476195 |
| Underweight | 15.65 | 14.60 | 7 | 21230 | 864 | 64476631 |
| Hyperhidrosis | 15.65 | 14.60 | 11 | 21226 | 124909 | 64352586 |
| Glomerulonephritis membranous | 15.62 | 14.60 | 8 | 21229 | 1332 | 64476163 |
| Fat tissue decreased | 15.61 | 14.60 | 4 | 21233 | 87 | 64477408 |
| Arthralgia | 15.49 | 14.60 | 84 | 21153 | 442176 | 64035319 |
| Asthma | 15.45 | 14.60 | 6 | 21231 | 95219 | 64382276 |
| Congestive cardiomyopathy | 15.38 | 14.60 | 18 | 21219 | 10326 | 64467169 |
| Lymphocytic infiltration | 15.27 | 14.60 | 8 | 21229 | 1396 | 64476099 |
| Progressive multifocal leukoencephalopathy | 15.27 | 14.60 | 24 | 21213 | 18208 | 64459287 |
| Giardiasis | 15.24 | 14.60 | 5 | 21232 | 265 | 64477230 |
| Acute haemorrhagic conjunctivitis | 15.23 | 14.60 | 3 | 21234 | 18 | 64477477 |
| Plagiocephaly | 15.23 | 14.60 | 3 | 21234 | 18 | 64477477 |
| Feeling abnormal | 15.17 | 14.60 | 13 | 21224 | 133589 | 64343906 |
| Hyperlipidaemia | 14.93 | 14.60 | 27 | 21210 | 22949 | 64454546 |
| Mitochondrial myopathy | 14.90 | 14.60 | 5 | 21232 | 284 | 64477211 |
| Anal cancer stage 0 | 14.70 | 14.60 | 3 | 21234 | 22 | 64477473 |
| Hepatitis acute | 14.66 | 14.60 | 20 | 21217 | 13369 | 64464126 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AJ01 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Integrase inhibitors |
| ATC | J05AR16 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HIV infections, combinations |
| FDA MoA | N0000000127 | HIV Integrase Inhibitors |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D019428 | HIV Integrase Inhibitors |
| MeSH PA | D019429 | Integrase Inhibitors |
| FDA EPC | N0000175887 | Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor |
| CHEBI has role | CHEBI:36044 | antiviral drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Human immunodeficiency virus infection | indication | 86406008 | DOID:526 |
| Disorder of muscle | contraindication | 129565002 | DOID:423 |
| Rhabdomyolysis | contraindication | 240131006 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.19 | acidic |
| pKa2 | 10.89 | acidic |
| pKa3 | 12.18 | acidic |
| pKa4 | 2.3 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 400MG BASE | ISENTRESS | MERCK SHARP DOHME | N022145 | Oct. 12, 2007 | RX | TABLET | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 400MG BASE | ISENTRESS | MERCK SHARP DOHME | N022145 | Oct. 12, 2007 | RX | TABLET | ORAL | 7435734 | Oct. 21, 2022 | INTEGRASE INHIBITION FOR THE TREATMENT OF HIV INFECTION |
| EQ 400MG BASE | ISENTRESS | MERCK SHARP DOHME | N022145 | Oct. 12, 2007 | RX | TABLET | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 600MG BASE | ISENTRESS HD | MERCK SHARP DOHME | N022145 | May 26, 2017 | RX | TABLET | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 600MG BASE | ISENTRESS HD | MERCK SHARP DOHME | N022145 | May 26, 2017 | RX | TABLET | ORAL | 7435734 | Oct. 21, 2022 | INTEGRASE INHIBITION FOR THE TREATMENT OF HIV INFECTION |
| EQ 600MG BASE | ISENTRESS HD | MERCK SHARP DOHME | N022145 | May 26, 2017 | RX | TABLET | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 25MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 25MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE/PACKET | ISENTRESS | MERCK SHARP DOHME | N205786 | Dec. 20, 2013 | RX | POWDER | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE/PACKET | ISENTRESS | MERCK SHARP DOHME | N205786 | Dec. 20, 2013 | RX | POWDER | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV INFECTION |
| 150MG;EQ 300MG BASE | DUTREBIS | MERCK SHARP DOHME | N206510 | Feb. 6, 2015 | DISCN | TABLET | ORAL | 7217713 | Oct. 21, 2022 | TREATMENT OF HIV-1 INFECTION |
| 150MG;EQ 300MG BASE | DUTREBIS | MERCK SHARP DOHME | N206510 | Feb. 6, 2015 | DISCN | TABLET | ORAL | 7435734 | Oct. 21, 2022 | TREATMENT OF HIV-1 INFECTION |
| EQ 400MG BASE | ISENTRESS | MERCK SHARP DOHME | N022145 | Oct. 12, 2007 | RX | TABLET | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV INFECTION |
| EQ 600MG BASE | ISENTRESS HD | MERCK SHARP DOHME | N022145 | May 26, 2017 | RX | TABLET | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV INFECTION |
| EQ 25MG BASE | ISENTRESS | MERCK SHARP DOHME | N203045 | Dec. 21, 2011 | RX | TABLET, CHEWABLE | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV INFECTION |
| EQ 100MG BASE/PACKET | ISENTRESS | MERCK SHARP DOHME | N205786 | Dec. 20, 2013 | RX | POWDER | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV INFECTION |
| 150MG;EQ 300MG BASE | DUTREBIS | MERCK SHARP DOHME | N206510 | Feb. 6, 2015 | DISCN | TABLET | ORAL | 7754731 | March 11, 2029 | TREATMENT OF HIV-1 INFECTION |
| EQ 600MG BASE | ISENTRESS HD | MERCK SHARP DOHME | N022145 | May 26, 2017 | RX | TABLET | ORAL | 10772888 | March 30, 2032 | TREATMENT OF HIV-1 INFECTION |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| C-C chemokine receptor type 1 | GPCR | Ki | 8.30 | CHEMBL | |||||
| Integrase | Enzyme | INHIBITOR | IC50 | 8 | CHEMBL | CHEMBL | |||
| Gag-Pol polyprotein | Polyprotein | INHIBITOR | IC50 | 7.52 | WOMBAT-PK | ||||
| Integrase | Enzyme | IC50 | 5.74 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D06676 | KEGG_DRUG |
| 871038-72-1 | SECONDARY_CAS_RN |
| 4026736 | VANDF |
| C1966407 | UMLSCUI |
| CHEBI:82960 | CHEBI |
| RLT | PDB_CHEM_ID |
| CHEMBL254316 | ChEMBL_ID |
| CHEMBL518520 | ChEMBL_ID |
| D000068898 | MESH_DESCRIPTOR_UI |
| DB06817 | DRUGBANK_ID |
| 11571 | IUPHAR_LIGAND_ID |
| 8842 | INN_ID |
| 22VKV8053U | UNII |
| 54671008 | PUBCHEM_CID |
| 1235585 | RXNORM |
| 121359 | MMSL |
| 24597 | MMSL |
| 31069 | MMSL |
| d07048 | MMSL |
| 012364 | NDDF |
| 012365 | NDDF |
| 1149432009 | SNOMEDCT_US |
| 429368003 | SNOMEDCT_US |
| 429707008 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0227 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0227 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0473 | TABLET, CHEWABLE | 25 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0473 | TABLET, CHEWABLE | 25 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0477 | TABLET, CHEWABLE | 100 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-0477 | TABLET, CHEWABLE | 100 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3080 | TABLET, FILM COATED | 600 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3080 | TABLET, FILM COATED | 600 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3603 | GRANULE, FOR SUSPENSION | 100 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0006-3603 | GRANULE, FOR SUSPENSION | 100 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1085 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-0650 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 28 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-0117 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-706 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 17 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61919-706 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 17 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66336-214 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67296-1235 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 18 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68071-2113 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 29 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1621 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 30 sections |
| ISENTRESS | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76519-1130 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 17 sections |