Agmatine
Aliases: 4-aminobutylguanidine, Decarboxylated arginine, 1-amino-4-guanidinobutane
Categories
Summary
Agmatine is an endogenous amine stored in synaptic vesicles and released on neuronal activation. It agonises imidazoline I1/I2 sites, inhibits NOS, and blocks NMDA receptor channels in a voltage-dependent manner, collectively producing mild anxiolysis, vascular smooth-muscle relaxation, and anti-addictive effects. Oral bioavailability is roughly 30%, with plasma half-life 75-120 min but brain/spinal half-life ~12 h, explaining why twice-daily split dosing maintains opioid-tolerance–reversal despite short plasma kinetics. Clinical and case data show chronic ingestion of 2.67 g/day for five years with normal lab values, yet forum users report tachyphylaxis of subjective effects after 2-3 weeks; cycling (2 weeks on / 1 week off) restores efficacy. For opioid harm-reduction, 500-1500 mg taken 1-2 h after the opioid appears to prolong analgesia and reduce required dose, whereas pre-dosing helps attenuate emerging tolerance.
Dose Information
| ROA | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| Oral (Capsule / Powder) | 100mg-400mg | - | - | - |
| Sublingual | 50mg-200mg | - | - | - |
| Rectal | 150mg-400mg | - | - | - |
Onset, Duration & After-effects
| ROA | Onset | Comeup | Peak | Offset | After Effects |
|---|---|---|---|---|---|
| Oral | 15-30 min | 30-60 min | 1-3 hrs | 2-4 hrs | 12 hrs |
| Oral (Capsule / Powder) | 15-45 min | 30-60 min | 1-2 hrs | 2-3 hrs | 6-12 hrs |
| Sublingual | 5-20 min | 20-45 min | 1-2 hrs | 2-3 hrs | 6-12 hrs |
| Rectal | 10-30 min | 30-60 min | 1-2 hrs | 2-3 hrs | 6-12 hrs |
Tolerance
Effects
- Anxiolysis
- Pain relief
- Stimulation
- Increased energy
- Insomnia
- Nausea
- Headache
- Vasodilation
- Stimulation or sedation
- Sedation
- Cognitive enhancement
- Mood enhancement
- Motivation enhancement
- Focus enhancement
- Stress reduction
- Emotional enhancement
- Memory enhancement
- Mild euphoria
- Anxiety suppression
- Emotion enhancement
- Empathy enhancement
- Addiction suppression
- Physical enhancement
- Light sensitivity
- Disinhibition
- Appetite suppression
- Spatial disorientation
- Derealization
- Dulled perception
- Visual distortions
- Visual disconnection
- Metallic taste