Pankaj Garkoti

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Pharmacokinetics and Subjective Effects of Pregabalin, Modafinil, and Piracetam

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Summary

Pregabalin, modafinil and piracetam each have well-characterized pharmacokinetics but distinct subjective effects. Pregabalin (Lyrica) is a CNS depressant (sedative/anxiolytic); modafinil is a wakefulness-promoting stimulant; piracetam is a “nootropic” with mild cognitive/energy effects. Below are detailed tables and timelines for each drug, combining clinical (half‑life, metabolism, dosing) and anecdotal reports (high-dose effects, subjective onset/peak/duration). Finally, a conceptual combined timeline illustrates the net sedation–alertness profile if all three are taken simultaneously (300 mg pregabalin + 200 mg modafinil + 2.4 g piracetam at time 0 by a healthy male with slight tolerance). All data points are sourced to clinical references and user reports where available.

Pregabalin (Lyrica)

Parameter Value / Range Source
Elimination half-life ~4.5–7 hours (mean ~6.3 h) Clinical studies
Excretion ~90% unchanged in urine (renal clearance ~67–81 mL/min) Primarily renal (unchanged drug)
Time to peak (Tmax) ~1.5 h (fast absorption) Pharmacokinetic data (fast, food-independent)
Typical dose 150–450 mg/day (divided) FDA-approved dosing
Max recommended dose 600 mg/day (IR) FDA limit; higher doses yield more adverse effects
High-dose reports Anecdotal up to 1,200 mg/day or more Erowid/Bluelight reports: euphoria/sedation at 600–1200 mg
Onset of subjective effects ~30–60 min (some sedation/anxiolysis) Clinical peak at 1.5 h, users report onset ~1 h
Peak subjective effects ~1–2 hours (sedation/dreaminess) Matches Tmax; users note peak euphoria/sedation by 1–2 h at high dose
Duration of effects ~6–8 hours (notable sedation/anxiolysis) Half-life ~6 h, effects wane by 8–12 h
Excretion time (elimination) ~5 half-lives ≈30–40 h (to negligible levels) ~5×t1/2 for ≈97% elimination

Notes: Pregabalin’s effects include sedation, anxiolysis and mild euphoria at higher doses. One user reported taking ~1050–1200 mg over 5 hours, feeling “loose” but still functional. Another noted 300 mg caused drowsiness and cognitive blurring. Tolerance often develops to euphoria, so some self-titers exceed 600 mg. Pregabalin’s C_max occurs ~1.5 h post-dose, consistent with onset ~1 h and peak ~1–2 h in reports. Effects generally wane after ~6–8 h, matching its ~6 h half-life.

Modafinil (Provigil)

Parameter Value / Range Source
Elimination half-life ~12–15 hours (R-modafinil ~10–17 h) Pharmacokinetic studies
Excretion ~80% urine (mostly inactive metabolite modafinil acid) Primarily hepatic metabolism; metabolites via urine
Time to peak (Tmax) ~2–4 h Clinical data (peak concentrations ~2–4 h after dose)
Duration of action ~10–12 h (therapeutic effect) Wakefulness effect ~half-life; referenced as ~11.5 h
Typical dose 100–200 mg once daily Standard medical dose
Max recommended dose 400 mg/day (acute studies; no added benefit >200) Up to 400 mg tolerated in narcolepsy studies; higher tends to add side effects
High-dose reports Occasional off-label use 400–600 mg/day Some patients on 400 mg; rare reports of 600+ mg
Onset of subjective effects ~30–60 min (alertness increase) Generally felt within 1 h; matches pharmacokinetics
Peak subjective effects ~2–4 hours (maximum alertness, focus) Aligns with Tmax; moderate cognitive enhancement and wakefulness reported
Duration of effects ~10–15 hours (carryover alertness) Consistent with long half-life; some lingering effect up to ~12–15 h
Excretion time ~5 half-lives ≈60–75 h (~3 days) ~5×t1/2 for near complete elimination

Notes: Modafinil promotes alertness and wakefulness without classic stimulant euphoria. It peaks slowly (~2–4 h) and lasts long (effects up to ~12 h). Clinical dosing is 100–200 mg, but studies show 400 mg/day is “well-tolerated” though with no extra benefit. A Bluelight user cautions “wouldn’t take more than 400 mg at a time”. Narcolepsy communities occasionally mention up to 600 mg/day or more, often with diminishing returns and some side effects (headache, irritability). Onset is within ~1 h, with focus/energy peaking ~2–3 h post-dose; effects persist through the day consistent with its long half-life.

Piracetam

Parameter Value / Range Source
Elimination half-life ~4–5 hours Clinical pharmacokinetic data
Excretion ~85–95% unchanged in urine Renal excretion of unchanged drug
Time to peak (Tmax) ~0.5–1.5 h “Peak plasma ~30–90 min after ingestion”
Typical dose 1,200–4,800 mg/day (in 2–3 doses) Common nootropic dosing range
High-dose reports 7–24 g/day (wide individual variation) Neurological use: 7–24 g/day dose-dependent; up to 45 g in special cases
Onset of subjective effects ~30–60 min (subtle cognition/energy) Rapid absorption; users report mild lift
Peak subjective effects ~1–2 hours (max cognitive/nootropic effect) Matches Tmax; some report sharper memory/alertness
Duration of effects ~4–6 hours (effects taper as drug is cleared) Half-life 4–5 h, so most effect gone by ~6 h
Excretion time ~5 half-lives ≈20–25 h (nearly complete) ~5×t1/2 ~1 day

Notes: Piracetam is a “racetam” nootropic, often taken in multi-gram doses. Clinically, doses of 7–24 g/day are used for cognitive disorders, and patients tolerated up to 45 g/day with notable benefits and minimal side effects. Among nootropic users, typical “supplement” doses are 1.6–4.8 g daily (divided), though some self-experiment with 6–10 g at once. Piracetam acts quickly (peak ~1 h), with subjective reports of increased mental clarity or mild stimulation rather than sedation. Effects generally last 4–6 h before declining as piracetam is eliminated (half-life ~5 h). Tolerance is reported low; side effects (headache, insomnia) are rare.

Individual Effect Timelines (at High Dose)

Based on the above data and high-dose reports, a typical timeline (onset, peak, offset) for each drug at near-maximal dose might be:

These are idealized for a “max dose” scenario; real experiences vary. For example, one user on 4800 mg/day reported noticeable cognitive lift by day 3. Another experimenter took 4.8 g daily for 3 days, then 2.4 g split doses, noting enhanced mood/energy.

Combined Effects (Three-Drug Timeline)

When all three are taken together (e.g. 300 mg pregabalin + 200 mg modafinil + 2.4 g piracetam at time 0), their effects overlap. Conceptually (see chart below), the alertness vs. time curve might look like this for a tolerant healthy male:

Subjective Experience and Practical Applications

What Users Would Feel

The combined experience of this three-drug cocktail creates a unique psychoactive profile that evolves throughout the day:

Early Phase (0-2 hours):

Peak Phase (2-4 hours):

Decline Phase (4-8 hours):

Late Phase (8+ hours):

Potential Use Cases

This combination might be particularly useful for:

Professional/Academic Applications:

Social Applications:

Therapeutic Considerations:

Important Considerations

Risks and Limitations:

Optimal Timing:

This combination essentially creates a “functional stimulation” profile - providing energy and focus while minimizing anxiety and overstimulation, making it potentially useful for demanding cognitive tasks in anxiety-provoking situations.

Sources

Pregabalin (Lyrica)

Modafinil (Provigil)

Piracetam