Peripherally selective drugPeripherally selective drugs have their primary mechanism of action outside of the central nervous system (CNS), usually because they are excluded from the CNS by the blood–brain barrier. By being excluded from the CNS, drugs may act on the rest of the body without producing side-effects related to their effects on the brain or spinal cord. For example, most opioids cause sedation when given at a sufficiently high dose, but peripherally selective opioids can act on the rest of the body without entering the brain and are less likely to cause sedation.
DomperidoneDomperidone, sold under the brand name Motilium among others, is a dopamine antagonist medication which is used to treat nausea and vomiting and certain gastrointestinal problems like gastroparesis (delayed gastric emptying). It raises the level of prolactin in the human body and is used to induce and promote breast milk production. It may be taken by mouth or rectally. Side effects of domperidone include headache, dry mouth, abdominal cramps, diarrhea, and elevated prolactin levels.
DynorphinDynorphins (Dyn) are a class of opioid peptides that arise from the precursor protein prodynorphin. When prodynorphin is cleaved during processing by proprotein convertase 2 (PC2), multiple active peptides are released: dynorphin A, dynorphin B, and α/β-neo-endorphin. Depolarization of a neuron containing prodynorphin stimulates PC2 processing, which occurs within synaptic vesicles in the presynaptic terminal. Occasionally, prodynorphin is not fully processed, leading to the release of “big dynorphin.
HyperalgesiaHyperalgesia (ˌhaɪpərælˈdʒiːziə or -siə; 'hyper' from Greek ὑπέρ (huper, “over”), '-algesia' from Greek algos, ἄλγος (pain)) is an abnormally increased sensitivity to pain, which may be caused by damage to nociceptors or peripheral nerves and can cause hypersensitivity to stimulus. Prostaglandins E and F are largely responsible for sensitizing the nociceptors. Temporary increased sensitivity to pain also occurs as part of sickness behavior, the evolved response to infection.
Opioid agonist therapyOpioid agonist therapy (OAT) is a treatment in which prescribed opioid agonists are given to patients who live with Opioid use disorder (OUD). The benefits of this treatment include a more manageable withdrawal experience, cognitive improvement, and lower HIV transmission. The length of OAT varies from one individual to another based on their physiology, environmental surroundings, and quality of life. The term medication for Opioid Use Disorder (MOUD) is used to describe medication including methadone and buprenorphine, which are used to treat patients with OUD.
NefopamNefopam, sold under the brand name Acupan among others, is a centrally acting, non-opioid painkilling medication, that is primarily used to treat moderate to severe pain. Nefopam acts in the brain and spinal cord to relieve pain via novel mechanisms: antinociceptive effects from triple monoamine reuptake inhibition, and antihyperalgesic activity through modulation of glutamatergic transmission. Nefopam is effective for prevention of shivering during surgery or recovery from surgery.
LevallorphanLevallorphan (INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartrate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia.
Insufflation (medicine)Insufflation (insufflare) is the act of blowing something (such as a gas, powder, or vapor) into a body cavity. Insufflation has many medical uses, most notably as a route of administration for various drugs. Gases are often insufflated into a body cavity to inflate the cavity for more workroom, e.g. during laparoscopic surgery. The most common gas used in this manner is carbon dioxide, because it is non-flammable, colorless, and dissolves readily in blood.
MethorphanMethorphan comes in two isomeric forms, each with differing pharmacology and effects: Dextromethorphan - An over-the-counter cough suppressant, as well as dissociative hallucinogen. Levomethorphan - A potent opioid analgesic that was never clinically developed; a prodrug of the powerful opioid agonist analgesic levorphanol (Levo-Dromoran). Racemethorphan is the racemic mixture of both of these stereoisomers.
MitragynineMitragynine is an indole-based alkaloid and the most abundant active alkaloid in the Southeast Asian plant Mitragyna speciosa, commonly known as kratom. The total alkaloid concentration in dried leaves ranges from 0.5 to 1.5%. In Thai varieties, mitragynine is the most abundant component (up to 66% of total alkaloids) while 7-hydroxymitragynine is a minor constituent (up to 2% of total alkaloid content). In Malaysian kratom varieties, mitragynine is present at lower concentration (12% of total alkaloids).
