for educational and safety purposes
Every compound in the sci-wiki that affects heart rate; the ones you can source are floated to the front, then the reference-only entries. Tap any for the full entry, mechanism, and outlets.
9 sourced · 3 reference
Atenolol is a beta-1 selective beta blocker, a cardiovascular drug that blocks the beta-1 adrenergic receptors of the heart. It is used to treat high blood pressure, angina, and certain irregular heart rhythms, and historically after heart attacks. Developed by Imperial Chemical Industries in the 1970s, it is water-soluble and crosses into the brain poorly, which tends to limit central nervous system side effects; many guidelines no longer list it as a first-choice treatment for uncomplicated high blood pressure.
Bisoprolol is a highly beta-1 selective adrenergic receptor antagonist, among the most cardioselective of the beta-blockers, taken once daily for hypertension, angina, certain arrhythmias and chronic heart failure. Its strong preference for cardiac beta-1 over pulmonary beta-2 receptors improves tolerability and permits cautious use even in many patients with coexisting airway disease. In the landmark CIBIS-II trial it reduced all-cause mortality and sudden cardiac death in stable heart failure with reduced ejection fraction, and the later CIBIS-III trial showed that beginning treatment with bisoprolol before an ACE inhibitor is a viable strategy. Individual-patient meta-analyses confirm the survival benefit of beta-blockade in patients in sinus rhythm while indicating attenuated benefit when atrial fibrillation coexists; bisoprolol appears on the World Health Organization list of essential medicines.
Ivabradine is a selective inhibitor of the hyperpolarization-activated funny current (If), carried largely by HCN4 channels in the sinoatrial node, which is the ionic current that sets the pace of the heartbeat. By slowing spontaneous diastolic depolarization it lowers heart rate without depressing myocardial contractility or blood pressure, distinguishing it from beta-blockers and calcium-channel blockers. In the SHIFT trial it reduced cardiovascular death and heart-failure hospitalization in patients with chronic systolic heart failure and elevated resting heart rate, whereas the BEAUTIFUL and SIGNIFY trials found no overall benefit in stable coronary disease without heart failure. Its precise action on sinus-node automaticity has also prompted off-label use in inappropriate sinus tachycardia and postural tachycardia syndrome; it was developed by Servier and reached markets in Europe in 2005 and the United States in 2015.
Metoprolol is a cardioselective beta-1 adrenergic antagonist that slows heart rate and reduces myocardial contractility and workload, lowering blood pressure and cardiac oxygen demand. It is among the most rigorously validated beta-blockers: the MERIT-HF trial demonstrated a significant mortality reduction in chronic heart failure, and, as a lipophilic agent, it reduces sudden cardiac death after myocardial infarction, an effect linked to central penetration and preservation of vagal tone. Its limits are equally well documented; the large POISE trial showed that routine perioperative use lowered myocardial infarction but increased stroke and total mortality, tempering enthusiasm for prophylactic beta-blockade. It is also effective for migraine prevention, and its metabolism by the polymorphic enzyme CYP2D6 contributes to marked interindividual variability now addressed by pharmacogenetic guidelines. It is available as the immediate-release tartrate and extended-release succinate salts.
Metoprolol succinate is the extended-release salt form of the cardioselective beta-1 blocker metoprolol, sold under the brand name Toprol-XL. Formulated to release slowly for once-daily dosing, it produces steady round-the-clock blockade of beta-1 adrenergic receptors, slowing the heart and lowering blood pressure. It is used for high blood pressure, angina, and, notably, chronic heart failure, where extended-release metoprolol has been shown to improve survival; it is distinguished from the immediate-release tartrate salt, and the two are not interchangeable.
Olmesartan medoxomil plus metoprolol is a fixed-dose tablet that combines an angiotensin II receptor blocker with a cardioselective beta blocker. It brings together olmesartan, which lowers blood pressure by relaxing blood vessels, and metoprolol, which slows the heart and reduces its workload by blocking beta-1 adrenergic receptors. The combination is used mainly for high blood pressure in patients who also benefit from a beta blocker, such as those with certain heart rhythm problems, angina, or a history of heart attack, and it is marketed as a single-pill product in countries including India.
Salbutamol, known as albuterol in the United States, is a short-acting beta-2 adrenergic receptor agonist used as a bronchodilator to open the airways. It is a mainstay reliever medication for asthma and chronic obstructive pulmonary disease, giving rapid relief of wheezing and breathlessness during flare-ups. Usually inhaled, it is sold under brand names such as Ventolin and appears on the World Health Organization's list of essential medicines [1].
Verapamil is a prescription medication of the calcium channel blocker class, specifically a non-dihydropyridine agent of the phenylalkylamine type. It is used to treat high blood pressure, angina and certain fast heart rhythms that arise above the ventricles, and it also serves as a first-line drug for preventing cluster headaches. Introduced in the 1960s, it works by slowing the movement of calcium into heart and blood-vessel cells.
Clenbuterol is used for fat loss, and that is the only reason most people encounter it, so it is worth being direct about what the evidence supports. It is a long-acting beta-2 agonist licensed in some countries as an asthma bronchodilator and widely used in veterinary medicine; it raises metabolic rate and drives lipolysis, and in livestock and rodents it reliably shifts body composition toward lean mass [32][31]. What is missing is the human version of that result. There is no controlled trial showing clenbuterol produces meaningful fat loss in healthy people, while there is a systematic review of case reports documenting what it does produce: tachycardia, arrhythmia, myocarditis and hospital admissions [14]. The gap between those two literatures is the whole story.
Guanfacine is a non-stimulant ADHD medication and a selective alpha-2A adrenergic receptor agonist, sold as extended-release Intuniv for ADHD and immediate-release Tenex for high blood pressure. It has no dopaminergic reward action and no abuse potential, but it lowers blood pressure and heart rate and must never be stopped abruptly because of rebound hypertension.
McN-A-343 is a quaternary muscarinic agonist that served for decades as the standard tool for identifying M1-mediated responses, and which is now understood to owe that apparent selectivity to uneven efficacy and to a second, allosteric binding site rather than to selective binding.
The fungal alkaloid that muscarinic receptors are named after; it has no therapeutic use and matters today as the toxin behind Inocybe and Clitocybe mushroom poisoning.