Collated from TripSit, Pharmacology, DrugCentral, DailyMed. Where sources differ (e.g. dosing), Compare shows them side by side.
Also known as inderal, hemangeol, innopranTS
Is a nonselective beta blocker. It is used in medication for high blood pressure, anxiety, and tremors. Also fun fact, it was the first successful beta-blocker developed.TS
Oral
Route dataTripSit
| Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| — | 10–30 mg | 40–80 mg | 80–140 mg | —+ |
| Onset | 10–45 minutes |
|---|---|
| Total | 3–7 hours |
| After-effects | 1–8 hours |
🧬 Receptor activityPHDC
| Target | Action | Affinity | Source | |
|---|---|---|---|---|
| Beta-2 adrenergic receptor | — | Ki 2.27 nM | CHEMBL | TargetBeta-2 adrenergic receptor Action— AffinityKi 2.27 nM SourceCHEMBL |
| Sigma non-opioid intracellular receptor 1 | — | Ki 95.38 nM | CHEMBL | TargetSigma non-opioid intracellular receptor 1 Action— AffinityKi 95.38 nM SourceCHEMBL |
| Sigma intracellular receptor 2 | — | Ki 352.9 nM | CHEMBL | TargetSigma intracellular receptor 2 Action— AffinityKi 352.9 nM SourceCHEMBL |
| 5-hydroxytryptamine receptor 6 | — | Ki 542 nM | CHEMBL | Target5-hydroxytryptamine receptor 6 Action— AffinityKi 542 nM SourceCHEMBL |
| 5-hydroxytryptamine receptor 1A | — | Ki 644.31 nM | CHEMBL | Target5-hydroxytryptamine receptor 1A Action— AffinityKi 644.31 nM SourceCHEMBL |
| 5-hydroxytryptamine receptor 2C | — | Ki 1373.1 nM | CHEMBL | Target5-hydroxytryptamine receptor 2C Action— AffinityKi 1373.1 nM SourceCHEMBL |
| 5-hydroxytryptamine receptor 2A | — | Ki 1790.2 nM | CHEMBL | Target5-hydroxytryptamine receptor 2A Action— AffinityKi 1790.2 nM SourceCHEMBL |
| Alpha-1B adrenergic receptor | — | Ki 10000 nM | CHEMBL | TargetAlpha-1B adrenergic receptor Action— AffinityKi 10000 nM SourceCHEMBL |
| Beta-1 adrenergic receptor (ADRB1) | Antagonist | 8.71 Ki | DRUGCENTRAL | TargetBeta-1 adrenergic receptor (ADRB1) ActionAntagonist Affinity8.71 Ki SourceDRUGCENTRAL |
| Beta-2 adrenergic receptor (ADRB2) | Antagonist | 8.25 Ki | DRUGCENTRAL | TargetBeta-2 adrenergic receptor (ADRB2) ActionAntagonist Affinity8.25 Ki SourceDRUGCENTRAL |
| Beta-3 adrenergic receptor (ADRB3) | Antagonist | 6.22 Ki | DRUGCENTRAL | TargetBeta-3 adrenergic receptor (ADRB3) ActionAntagonist Affinity6.22 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 1A (HTR1A) | — | 6.913 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 1A (HTR1A) Action— Affinity6.913 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 1B (HTR1B) | — | 6.197 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 1B (HTR1B) Action— Affinity6.197 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 1D (HTR1D) | — | 5.346 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 1D (HTR1D) Action— Affinity5.346 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 2A (HTR2A) | — | 5.378 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 2A (HTR2A) Action— Affinity5.378 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 2B (HTR2B) | — | 6.662 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 2B (HTR2B) Action— Affinity6.662 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 2C (HTR2C) | — | 5.92 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 2C (HTR2C) Action— Affinity5.92 Ki SourceDRUGCENTRAL |
| 5-hydroxytryptamine receptor 6 (HTR6) | — | 5.847 Ki | DRUGCENTRAL | Target5-hydroxytryptamine receptor 6 (HTR6) Action— Affinity5.847 Ki SourceDRUGCENTRAL |
| Adrenergic receptor beta (Adrb2) | — | 8.62 Ki | DRUGCENTRAL | TargetAdrenergic receptor beta (Adrb2) Action— Affinity8.62 Ki SourceDRUGCENTRAL |
| Beta-1 adrenergic receptor (Adrb1) | — | 8.52 Ki | DRUGCENTRAL | TargetBeta-1 adrenergic receptor (Adrb1) Action— Affinity8.52 Ki SourceDRUGCENTRAL |
| Beta-2 adrenergic receptor (Adrb2) | — | 9.01 Kd | DRUGCENTRAL | TargetBeta-2 adrenergic receptor (Adrb2) Action— Affinity9.01 Kd SourceDRUGCENTRAL |
| Cytochrome P450 1A2 (CYP1A2) | — | 5.398 IC50 | DRUGCENTRAL | TargetCytochrome P450 1A2 (CYP1A2) Action— Affinity5.398 IC50 SourceDRUGCENTRAL |
| Cytochrome P450 2D6 (CYP2D6) | — | 5.699 IC50 | DRUGCENTRAL | TargetCytochrome P450 2D6 (CYP2D6) Action— Affinity5.699 IC50 SourceDRUGCENTRAL |
| D(2) dopamine receptor (Drd2) | — | 4.89 Ki | DRUGCENTRAL | TargetD(2) dopamine receptor (Drd2) Action— Affinity4.89 Ki SourceDRUGCENTRAL |
| Histamine H1 receptor (HRH1) | — | 4.699 Ki | DRUGCENTRAL | TargetHistamine H1 receptor (HRH1) Action— Affinity4.699 Ki SourceDRUGCENTRAL |
| Membrane-associated progesterone receptor component 1 (Pgrmc1) | — | 5.671 Ki | DRUGCENTRAL | TargetMembrane-associated progesterone receptor component 1 (Pgrmc1) Action— Affinity5.671 Ki SourceDRUGCENTRAL |
| Multidrug resistance protein 1 (ABCB1) | — | 4.32 Ki | DRUGCENTRAL | TargetMultidrug resistance protein 1 (ABCB1) Action— Affinity4.32 Ki SourceDRUGCENTRAL |
| Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (HCN4) | — | 4.297 IC50 | DRUGCENTRAL | TargetPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (HCN4) Action— Affinity4.297 IC50 SourceDRUGCENTRAL |
| Sigma non-opioid intracellular receptor 1 (SIGMAR1) | — | 5.919 Ki | DRUGCENTRAL | TargetSigma non-opioid intracellular receptor 1 (SIGMAR1) Action— Affinity5.919 Ki SourceDRUGCENTRAL |
| Sodium-dependent serotonin transporter (SLC6A4) | — | 6.695 Ki | DRUGCENTRAL | TargetSodium-dependent serotonin transporter (SLC6A4) Action— Affinity6.695 Ki SourceDRUGCENTRAL |
| Solute carrier family 22 member 1 (SLC22A1) | — | 4.2 IC50 | DRUGCENTRAL | TargetSolute carrier family 22 member 1 (SLC22A1) Action— Affinity4.2 IC50 SourceDRUGCENTRAL |
| Voltage-dependent L-type calcium channel subunit alpha-1C (CACNA1C) | — | 4.319 Ki | DRUGCENTRAL | TargetVoltage-dependent L-type calcium channel subunit alpha-1C (CACNA1C) Action— Affinity4.319 Ki SourceDRUGCENTRAL |
Mechanism of actionPHDM
Propranolol is a nonselective β-adrenergic receptor antagonist. Blocking of these receptors leads to vasoconstriction, inhibition of angiogenic factors like vascular endothelial growth factor (VEGF) and basic growth factor of fibroblasts (bFGF), induction of apoptosis of endothelial cells, as well as down regulation of the renin-angiotensin-aldosterone system.
PharmacodynamicsPH
Propranolol is a beta-adrenergic receptor antagonist used to treat hypertension. Propranolol has a long duration of action as it is given once or twice daily depending on the indication. When patients abruptly stop taking propranolol, they may experience exacerbations of angina and myocardial infarctions.
Pharmacokinetics
Half-lifePH
The elimination half-life of propranolol is approximately 8 hours. The plasma half-life of propranolol is 3 to 6 hours.
AbsorptionPHDM
Patients taking doses of 40mg, 80mg, 160mg, and 320mg daily experienced Cmax values of 18±15ng/mL, 52±51ng/mL, 121±98ng/mL, and 245±110ng/mL respectively. Propranolol has a Tmax of approximately 2 hours, though this can range from 1 to 4 hours in fasting patients. Taking propranolol with food does not increase Tmax but does increase bioavailability.
91% of an oral dose of propranolol is recovered as 12 metabolites in the urine.
The volume of distribution of propranolol is approximately 4L/kg or 320L.
The clearance of propranolol is 2.7±0.03L/h/kg in infants <90 days and 3.3±0.35L/h/kg in infants >90 days. Propranolol clearance increases linearly with hepatic blood flow. Propranolol has a clearance in hypertensive adults of 810mL/min.
MetabolismPHDM
Propranolol undergoes side chain oxidation to α-naphthoxylactic acid, ring oxidation to 4’-hydroxypropranolol, or glucuronidation to propranolol glucuronide. It can also be N-desisopropylated to become N-desisopropyl propranolol. 17% of a dose undergoes glucuronidation and 42% undergoes ring oxidation.
Propranolol has known human metabolites that include (2S,3S,4S,5R)-3,4,5-Trihydroxy-6-[1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-yl]oxyoxane-2-carboxylic acid.
Protein bindingPHDM
Approximately 90% of propranolol is protein bound in plasma. Other studies have reported ranges of 85-96%.
Plan a dose of Propranolol
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External links
Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.