Liletta
Liletta
Generic Name
Liletta
Mechanism
- Selective inhibition of renal SGLT2:
- Blocks ~90 % of glucose reabsorption in the proximal tubule.
- Lowers post‑renal threshold → glucosuria and negative glucose balance.
- Keeps insulin‑independent, enabling use in insulin‑deficient states.
- Lowers hemoglobin A1c (HbA1c) and fasting plasma glucose (FPG) by ~0.5–0.7 % and ~1 mmol/L, respectively.
Pharmacokinetics
| Parameter | Typical Value | Notes |
| Route | Oral | Tablets |
| Absorption | Tmax ≈ 3 h; F ≈ 70 % (food does not affect exposure significantly) | Moderate inter‑individual variability |
| Distribution | Vd ≈ 400 L; limited protein binding (~80 %) | Steady‑state achieved ~5 days |
| Metabolism | Predominantly CYP3A4/5 & CYP1A2; minor CYP2C9 | Metabolites inactive |
| Elimination | Renal (≈ 55 %) and intestinal fecal routes | Excretion half‑life 10–12 h |
| Dose‑adjustment | Lower dose if eGFR < 45 mL/min/1.73 m²; avoid if eGFR < 30 | No adjustment for mild‑to‑moderate hepatic impairment |
Indications
- Adjunctive oral therapy with diet/exercise for adult patients with T2DM.
- Optional addition to insulin or basal‑bolus regimes when glycemic targets are unmet.
Contraindications
- Contraindicated in type 1 diabetes (risk of ketoacidosis) and diabetic ketoacidosis (DKA) in any etiology.
- Kidney function: avoid if eGFR < 30 mL/min/1.73 m²; reduce dose for eGFR 30–45 mL/min/1.73 m².
- Pregnancy: category D – not recommended.
- Caution with medications that may influence renal perfusion (e.g., NSAIDs, ACEi/ARB) due to potential for acute kidney injury.
- Genital & UTI risk: elevated in women; monitor for signs of infection.
- Hypotension: risk in volume‑depleted states (e.g., elderly, diuretics, vomiting).
- Euglycemic DKA: silent DKA risk; educate on symptoms (abdominal pain, nausea, ketones).
Dosing
- Initial dose: 12.5 mg orally once daily (QD) in the morning.
- Titration: If glycemic targets unmet after 6 weeks, increase to 25 mg QD.
- Post‑titration: May be taken with or without food, but consistent timing improves adherence.
- Switching: Gradual taper of preceding antidiabetics (e.g., metformin) if needed to avoid hypoglycemia.
- Missed dose: Take as soon as remembered; do not double dose.
Adverse Effects
| Adverse Effect | Incidence (Clinical Trials) | Comment |
| Genital mycotic infections (vaginal candidiasis, balanitis) | ~5–7 % | Topical antifungals first line |
| Urinary tract infections | ~3–5 % | Reassess causative pathogens |
| Volume depletion/hypotension | < 2 % | Check orthostatic vitals post‑initiation |
| Dizziness / headache | < 5 % | Educate on postural changes |
| Euglycemic DKA | < 1 % | Severe case; monitor ketones in prodromal patients |
| Rare: fractures, acute kidney injury | < 0.5 % | Use caution in osteoporosis or CKD patients |
| Gastrointestinal: nausea, diarrhoea | < 5 % | Usually mild, transient |
Monitoring
| Parameter | Frequency | Rationale |
| HbA1c | Every 3 – 6 weeks initially, then q3–6 mo | Evaluate efficacy |
| Fasting glucose | Every 2–3 weeks until stable | Detect hypoglycemia risk |
| eGFR/serum creatinine | Every 3 months (or sooner if volume‑status changes) | Adjust dose or discontinue |
| Ketones | When symptomatic or in high‑risk patients | Prevent DKA |
| Blood pressure | At each visit | Volume‑status surveillance |
| Urinalysis | At baseline and every 6–12 months | Detect occult hematuria or infection |
Clinical Pearls
- Start Low, Go Slow: In patients with baseline eGFR 30–45 mL/min, begin with 12.5 mg; if tolerated, step to 25 mg only after 6 weeks.
- Volume Status Matters: Educate patients on adequate hydration, especially when concurrently on loop diuretics or in hot climates.
- DKA Vigilance: Pregnant, post‑surgical, or fasting (e.g., Ramadan) patients need ketone checks before and after therapy.
- SGLT2 + GLP‑1 Co‑therapy: The combination provides additive weight loss and HbA1c reduction, yet monitor for additive GI side‑effects.
- Safety in CKD: Though glycemic efficacy declines with eGFR < 45, continuing the drug for cardiovascular benefits is acceptable; monitor cardiovascular events closely.
- Patient Education: Provide written instructions on signs of genital infection and when to seek care; include hand‑washing guidelines to prevent antifungal spread.
--
• *This drug card is derived from peer‑reviewed clinical studies and FDA labeling. Refer to the latest prescribing information for updates.*