obidoxime chloride [INN, USAN] (HS-3) is an oxime CHOLINESTERASE REACTIVATOR.

It can be used parenterally as an ANTIDOTE adjunct to atropine in treating human or animal (organophosphate group) ANTiCHOLINESTERASE pesticide toxicity. Occlusal * salicylic acid. OCiltide [INN] (Hoe 825) is an enkephalin peptide derivative, a peripheral-acting mixed u/8 OPIOID RECEPTOR AGONIST, which is reported to have (paradoxical) gut and GASTRIC MOTILITY STIMULANT actions. ocrase [INN] is a proteolytic ENZYME with FIBRiNOLYTiC activity, thus acting as a THROMBOLYTIC. Chemically, it is isolated from the mould Aspergillus ochraceus. Therapeutically, it can be used to treat thrombolytic disease. OCtabenzone [INN, USAN] is a benzophenone, a SUNSCREEN AGENT. octacaine [INN] is a LOCAL ANAESTHETIC which has been used by topical application for local pain relief. It has ANTIARRHYTHMIC properties. OCtacosactrin [BAN] (tosactide [INN]) is a synthetic peptide, a structural CORTICOTROPHIN ANALOGUE (the first 28 amino acids of human corticotrophin), which has been used clinically.

octastatin vapreotide.
octatropine methyl bromide [BAN, INN] (anisotropine methylbromide [JAN, USAN]) is a quaternary ammonium
MUSCARINIC CHOLINOCEPTOR ANTAGONIST, which can be used

as a visceral ANTiSPASMODiC AGENT and as an adjunct in the treatment of peptic ulcer. octenidine [BAN, INN] (octenidine hydrochloride [USAN]) is a quaternary ammonium compound with ANTIFUNGAL and ANTIBACTERIAL activity. It can be used as a topical antiinfective and dental plaque inhibitor.

octenidine hydrochloride * octenidine.

OCtOCOQ alfa [BAN] (Kogenate; Recombinate) is a recombinant form of blood coagulation factor VIII. It is used in the treatment of haemophilia A. octocrilene [INN] (octocrylene [USAN]) is a cinnamic acid derivative. It can be used in topical SUNSCREEN preparations.

octocrylene octocrilene. octodecactide + codactide

octodrine [INN, USAN] is a VASOCONSTRICTOR that formerly was used in the treatment of hypotensive states. octopamine [INN] (norsynephrine; noroxedrine) is a phenylethylamine alkaloid from Capsicum frutescens, Citrus spp., Cyperusspp. (Solanaceae, Rutaceae, Cyperaceae). It occurs in many animal tissues; found in high concentrations in the posterior salivary gland of Octopus vulgaris. It serves as an invertebrate neurotransmitter. It is predominantly an a-ADRENOCEPTOR AGONIST, and has been used as a hypertensive to treat hypotensive states. Octopressin felypressin. OCtOtiamine [INNJAN] is a long-acting oral thiamine VITAMIN analogue (vitamin B1 source).
SMALL CAPS = drug families (by mechanism or application)

Octreoscan - pentetreotide. OCtreotide [BAN, INN, USAN] (octreotide acetate [USAN]; SMS 201-995; Sandostatin) is a long-lasting analogue of the HYPOTHALAMlC HORMONE somatostatin (hypothalamic release-inhibiting hormone), and is a SOMATOSTATIN RECEPTOR AGONIST. It is a growth hormone secretion inhibitor and can be used in the short-term treatment of acromegaly. It is used by injection as an adjunct in ANTICANCER treatment for the relief of symptoms caused by the release of hormones from carcinoid tumours of the endocrine system, including VIPomas and glucagonomas. octreotide acetate * octreotide. Ocufen flurbiprofen. Ocusert Pilo pilocarpine. ODA 914 demoxytocin. Odrik <* trandolapril. oestradiol [BAN] (estradiol [INN, USAN]; oestradiol benzoate [BAN]; estradiol benzoate [INN]; estradiol hexahydrobenzoate [INN]; ostradiol dipropionate [BAN]; estradiol cypionate [INN]; estradiol valerate [INN, USAN]; oestradiol valerate [BAN]; estradiol enanthate [INN, USAN]; Climaval; Elleste-Solo; Estraderm; Estring; Evorel; Fematrix; Menorest; Oestrogel; Progynova; Vagifem; Zumenon) was originally isolated from ovaries and pregnancy urine, and is the most potent of the natural OESTROGENS. Oestradiol and its semisynthetic esters are used extensively in oestrogen replacement therapy, often in combination with PROGESTOGENS. oestradiol benzoate - oestradiol. oestradiol valerate oestradiol. Oestrifen *tamoxifen. oestriol (estriol; NSC 12169; oestriol succinate [BAN]; estriol succinate [INN]; estriol acetate benzoate [JAN]; NSC 12169; Ortho-Gynest; Ovestin and many other names) is a naturally occurring steroid, an OESTROGEN that is used orally or topically in oestrogen replacement therapy (sometimes in combination with a PROGESTOGEN) to treat menstrual, menopausal or other gynaecological problems (including infertility). oestriol succinate * oestriol. Oestrogel ^ oestradiol. oestrogens (estrogens, USA) is the name given to the group of steroid sex hormones that promote the growth and functioning of the female sex organs and the development of female sexual characteristics. In their natural forms they are produced and secreted mainly by the ovary, and to a small extent by the placenta of pregnant women, the adrenal cortex and in men the testes. The three main natural oestrogens are oestradiol, oestrone and oestriol. Natural and synthesized oestrogens are used therapeutically, sometimes in combination with PROGESTOGENS, to treat menstrual, menopausal (e.g. HRT) or other gynaecological problems. Some synthetic oestrogens are also used to treat certain cancers (e.g. prostate and breast cancer), and also postmenopausal osteoporosis (see ANTICANCER AGENTS). A major use of oestrogens is as oral CONTRACEPTIVES (nomally in combination with progesterones). Oestrogens work by binding at intracellular receptors, and the interaction of the resultant complexes with nuclear sites results in genomic effects. These effects may be gene transcription (DNA-directed RNA and protein synthesis), or gene repression (inhibition of transcription). Oestrogen receptors are found at many sites, but notably in the reproductive system (e.g. breasts, uterus, vagina). One effect of oestrogens on DNA is the induction of synthesis of
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

progesterone receptors on tissues, such as uterus and vagina, and posterior pituitary and hypothalamus. Best-known and most-used oestrogens are estradiol, estriol, ethinyloestradiol, mestranol and stilbestrol (stiiboestrol). ANTlOESTROGENS include tamoxifen which binds to oestrogen receptors with little stimulation, so acts as an antagonist; used to treat oestrogen-dependent breast cancer.
Chaudhury, R.R. (1981) Pharmacology of estrogens, in International Encyclopedia of Pharmacology and Therapeutics. Pergamon Press, Oxford, section 106. Jacobs, H.S. et al. (1992) Postmenopausal hormone replacement therapy. Br. Med. /., 305,1403-1408. Whitcroft, S.I.J. era/. (1992) Hormone replacement therapy: risks and benefits. Clin. Endocrinol., 36,15-20. Belchetz, RE. (1994) Hormonal treatment of postmenopausal women. N. Engl. J. Med., 330,1062-1071.

oestrone [BAN] (estrone [INN]; follicular hormone; oxohydroxyoestrin; Kestrin and many other names) is a natural steroid OESTROGEN, obtained from pregnant women's urine and pregnant mares' urine. It is used therapeutically in combination with other natural oestrogens mainly in HRT. Its O-sulphate piperazine salt is estropipate. Ofloxacin [BAN, INN, JAN, USAN] (Exocin, Floxin; Tarivid etc.) the racemate is ofloxacin; the (S) -form is levofloxacin [BAN, INN, USAN]. It is an ANTIMICROBIAL, one of a 4-quinolone family related to nalidixic acid, which, though synthetic agents, are sometimes regarded as ANTIBIOTICS. It can be used as a wide-spectrum ANTIBACTERIAL used orally or systemically against Gram-positive and -negative bacterial infections. Ogen ^ estropipate. ohmefentanyl (RTl 4614-4) is one of the phenylpiperidine series and a fentanyl analogue, a (u) OPIOID RECEPTOR AGONIST with OPIOID ANALGESIC activity. oil of winter green ~ methyl salicylate Okadaic acid is a polyether derivative of a 38-carbon fatty acid elaborated by marine dinoflagellates and accumulated in sponges and in mussels (Halichondria okadai). It acts as a selective inhibitor of protein phosphatase-1 and -2A, and is used as a pharmacological and biochemical tool. OKT3 muromonab-CD3. OL 1 thioxolone. OL 110 thioxolone.
Olanzapine [BAN, INN, USAN] (LY 170053; Zyprexa) is a

[l,5]benzodiazepine, a (5HT2) 5-HYDROXYTRYPTAMINE

RECEPTOR ANTAGONIST and a (D2) DOPAMINE RECEPTOR

ANTAGONIST, recently introduced as an ANTiPSYCHOTiC, used orally to tranquillize patients suffering from schizophrenia and other acute and chronic psychotic disorders. Olbetam ~acipimox. oleandomycin [BAN, INN] is a (macrolide) ANTIBIOTIC with broad-spectrum ANTIBACTERIAL and ANTIMICROBIAL activity. oleovitamin D2 ergocalciferol. olopatadine [INN] (olopatadine hydrochloride [USAN]; KW 4679; AL 4943A) is a dibenzoxepin acetic acid, a novel mediator release inhibitor and HISTAMiNE Hi-RECEPTOR ANTAGONIST. It can potentially be used as an ANTIALLERGIC AGENT in the treatment of allergic rhinitis, urticaria, allergic conjunctivitis and asthma. olopatadine hydrochloride ~ olopatadine.
olsalazine [BAN, INN] (olsalazine sodium [BAN, USAN]; sodium azodisalicylate; Dipentum) is metabolized in vivo to

5-aminosalicylic acid (5-ASA), one of the aminosalicylate

group Of ANTIINFLAMMATORY and ANTICOLITIS AGENTS used for

ulcerative colitis. It is also a dye, mordant yellow. olsalazine sodium olsalazine.

olvanil [INN, USAN] (A/-vanillyloleamide) isacapsaicin

analogue regarded as a VANILLOID RECEPTOR AGONIST. It can be

SMALL CAPS = drug families (by mechanism or application)

used as an ANTHNFLAMMATORY, antinociceptive agent and non-narcotic ANALGESIC. Strictly, the name olvanil applies to the (Z) -form. OM 1563 ~ pyrithione zinc, omadine ^ pyrithione zinc, omadine disulfide * dipyrithione. omadine MDS bispyrithione magsulfex. omega-3 marine triglycerides [BAN] (Maxepa) is a mixture of fatty acid triglycerides (from marine fish), containing 18% of 5,8,11,14,17-eicosapentaenoic acid (EPA) and 12% of 4,7,10,13,16,19-docosahexaenoic acid (DHA; deconexent; cervonic acid). Omega-3 fatty acids are longchain polyunsaturated fatty acids, and the parent fatty acid of this group, alpha-linolenic acid, an essential fatty acid that the body is unable to synthesize, can be converted in the body to EPA and DHA. The triglycerides act as ANTIHYPERLIPIDAEMICS that reduce plasma triglycerides and are used as a dietary supplement. It is a component of many preparations. 7-omen menogaril. omeprazole [BAN, INNJAN, USAN] (omeprazole sodium [USAN]; Losec; Prilosec) is a substituted benzimidazole, a GASTRIC PROTON PUMP INHIBITOR, a (H+/K+) ATPASE INHIBITOR. It can be used as an ANTIULCEROGENIC in the treatment of gastric ulcers and other gastric acid-related gastrointestinal disorders. It can be used in combination with amoxicillin for eradication of gastric Helicobacter pylori infection. omeprazole sodium * omeprazole. Omnipen ampicillin. omoconazole [INN] is an (imidazole group) ANTIFUNGAL, which can be used systemically or orally to treat a range of fungal infections. onapristone [INN] is a synthetic steroid derivative, which acts as a progestogen hormone antagonist and is used as an ABORTIFACIENT; also has antiglucocorticoid activity. Oncaspar pegaspargase. Oncovin ^ vincristine. ondansetron [BAN, INN] (ondansetron hydrochloride [BAN]; Zofran) is a substituted imidazolylcarbazolone, a selective (5-HT3) 5-HYDROXYTRYPTAMINE RECEPTOR ANTAGONIST. It shows ANTIEMETIC and antinauseant activity against anticancer radiotherapy or chemotherapy induced emesis. ondansetron hydrochloride ondansetron. One-Alpha * alfacalcidol ONO 802 * gemeprost. ONO 995 ~ froxiprost ONO 1052 * delprostenate. ONO 3708 is a prostaglandin derivative, a (thromboxane; TP) PROSTANOlD RECEPTOR ANTAGONIST. It has experimental hepatoprotective properties. Ontazolast [USAN] (BlRM 270) is a pyridinylbenzoxazolamine derivative, a LiPOXYGENASE INHIBITOR with potential ANTIASTHMATiC activity. OPC 21268 is a quinolinone derivative, a selective (V1 subtype) VASOPRESSiN RECEPTOR ANTAGONIST, with ANTIHYPERTENSlVE properties. OPC 12759 * rebamipide. Opilon ^ thymoxamine. OPIOID ANALGESICS (narcotic analgesics) are ANALGESICS typified by morphine. They have powerful actions on the CNS, and act to alter the perception of pain. Because of the numerous possible side-effects, the most important of which is dependence, such agents are usually used under strict medical supervision and are normally only available on prescription. Other notable side-effects include depression of respiration, nausea and vomiting, sometimes
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

hypotension, constipation (see ANTIDIARRHOEAL AGENTS), inhibition of coughing (see ANTITUSSIVES) and constriction of the pupils (miosis). See also NSAID ANALGESICS. Opiates, as a group, are derived from opium, an exudate from the ripe poppy Papaver somniferum. It contains many pharmacologically active alkaloids, of which there are two main chemical types: the benzylisoquinoline series (e.g. papaverine); and the phenanthrene series. The original opiate analgesics isolated from opium are phenanthrenes, including, along with morphine itself, codeine and thebaine. The only remaining medically used opium preparation is papaveretum (Omnopon), which is a mixture of alkaloids. Tens-of-thousands of semisynthetic opiate derivatives have been tested in an attempt to improve the pharmacological profile and reduce propensity to drugdependence. The first, diamorphine (heroin), was originally introduced in 1898, but though marginally more potent than morphine, it is dangerously habituating. Chemically, more distantly related synthetic opiates have been developed, such as the phenylpiperidine series (pethidine and fentanyl), and the methadone series (e.g. methadone and dextropropoxyphene) - both of which are regularly used in medicine, though they are less potent than morphine. The thebaine series (e.g. buprenorphine) is more closely related to morphine, and some members are a great deal more potent than morphine itself. The benzomorphan series (e.g. pentazocine) has rather different properties (see below). These heterocyclic opioid agents, with a diverse structure, act by binding to one or more of the opioid receptor sites which are to be found on neural (and some other sites) in the central and peripheral nervous systems. It is now recognized that these are the natural receptor sites for recognition of the endogenous members of the peptide opioid neurotransmitters families, which are found in neuronal tissue of the brain and elsewhere. There are three families of peptides (which are products of different genes): the enkephalins (principally from preproenkephalin); endorphins (from preproopiomelanocortin; POMC); and dynorphins (from preprodynorphin or preproenkephalin B). There are also at least three receptor types, \i (mu), K (kappa) and 8 (delta), again each controlled by a distinct gene. The receptors are all of the seven-transmembrane G-protein-coupled receptor superfamily, and have largely inhibitory effects on neuronal excitability - by means of opening potassium channels or closing calcium-channels - via a G-protein component negative-coupled to adenylyl cyclase pathway (see OPIOID RECEPTOR AGONISTS; POTASSIUM-CHANNEL ACTIVATORS; POTASSIUM-CHANNEL BLOCKERS). Each of these three receptor subtypes can cause analgesia, and there is no exclusive relationship between peptide family and the receptor subtype activated. In terms of medicinal chemistry, development of bioassay systems capable of independently measuring potency, or affinity, at each of the receptor subtypes, has facilitated a number of initiatives designed to find desirable combinations of agonist, partial agonist or competitive antagonist activities (in one molecule). The main objectives have been to improve on the potency and pharmacological profile of morphine, whilst minimizing the habituating liability. This has not been entirely successful, but some mixes of activity at \i and K receptors - of agonist, partial agonist or even antagonist activity - seem useful. Such mixed analgesics (e.g. buprenorphine, cyclazocine, meptazinol and pentazocine) have entered medicine as analgesics with limited tendency to cause drug-dependence or abuse
SMALL CAPS = drug families (by mechanism or application)

potential. However, some opioids, including the benzomorphans (e.g. pentazocine and cyclazocine), bind appreciably to a further site, the a (sigma) receptors that, unlike the opioid receptors detailed, have psychotomimetic potential, so patients may experience hallucinations. The o-site is best not classed as an opioid receptor site, as it is not blocked by normal opioid antagonists such as naloxone - a fact of clinical importance. Also, recently, an 'orphan' receptor (ORL1) of a further form has been demonstrated, and it binds a dynorphin-like heptapeptide sequence termed nociceptin (or orphanin-FQ). The applications of this finding remain to be seen. A number of potent antagonists acting at p., K or 6 receptors are available, and are useful for reversing opioid effects in medicine or in abuse overdose (e.g. naloxone), or in treating drug dependence (naltrexone): see OPIOID RECEPTOR ANTAGONISTS. Some weaker opioids are used as ANTITUSSIVES (e.g. codeine, dextromethorphan and pholcodine) or as ANTIDIARRHOEAL AGENTS (e.g. loperamide). Several peptide opioids have been developed as analgesics or antitussives (e.g. BW 443C81), but none has proved strikingly successful. There have been attempts to develop analgesic agents that work indirectly, through interfering with the breakdown of natural opioids in the body. Experimentally, some peptidase inhibitors have been shown to have analgesic actions; mainly a combination of thiorphan (an inhibitor of NEP (enkephalinase') and bestatin (an inhibitor of aminopeptidase B: see AMINOPEPTIDASE INHIBITORS; NEUTRAL
ENDOPEPTIDASE INHIBITORS.

There have been extensive searches for alternative analgesics acting on the nervous system without addictive and other side-effects, and there are some areas of promise. One initiative is to target the same cellular mechanism of action as the opioids (an inhibitory effect on neuronal excitability by opening potassium channels or closing calcium channels, through receptors negatively coupled to adenylyl cyclase), but with non-opioids. Here compounds which enhance actions at cc2-adrenoceptor, or certain 5-HT receptors, show promise. The ct2-adrenoceptor agonist clonidine is used as an analgesic in veterinary practice. Tramadol is a novel analgesic, used clinically as a racemic combination of two enantiomers, with a mix of fi-opioid and central monoaminergic activities (5-HT and noradrenaline reuptake inhibitor).
Herman, Nl. etal. (1990) Extradural opioids in labour. Br. J. Anaesth., 64. 528-529. Millan, M.J. (1990) K-Opioid receptors and analgesia. Trends Pharmacol. ScL, 11, 7076. Hoskin, RJ. et al. (1991) Opioid agonist-antagonist drugs in acute and chronic pain states. Drugs, 41, 326-344. Schug, S.A. etal. (1992) Pharmacological management of cancer pain. Drugs, 43, 44-53. Takemori, A.E. etal. (1992) Selective naltrexone-derived opioid receptor antagonists. Annu. Rev. Pharmacol. Toxicol., 32, 239-269. Pasternak, G.W. (1993) Pharmacological mechanisms of opioid analgesics. CUn. Neuropharmacol., 16,1-18.

OPIOID RECEPTOR AGONISTS bind at, and activate, one or more of the subtypes of receptor that recognize the endogenous peptide opioids. Agonist ligands notably include plant alkaloids, such as morphine, and also diverse synthetic heterocyclic derivatives. These are used for a number of purposes, principally as narcotic analgesics. Their use is discussed in more detail under other headings: see ANTIDIARRHOEAL AGENTS; ANTITUSSIVES; OPIOID ANALGESICS. Very large numbers of synthetic heterocyclic opioid receptor agonists have now been synthesized, and there is a considerable body of evidence about structure-activity relationships. Opiates, as a group, are derived from opium,
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

an exudate from the ripe poppy Papaver somniferum. It contains many pharmacologically active alkaloids, of which the phenanthrene series includes, along with morphine itself, codeine and thebaine. Tens-of-thousands of semisynthetic opiate derivatives have been tested in an attempt to improve the pharmacological profile and reduce propensity to drugdependence. These include diamorphine (heroin) and chemically more distantly related synthetic opiates, such as the phenylpiperidine series (pethidine and fentanyl) and the methadone series (e.g. methadone and dextropropoxyphene); both of which are regularly used in medicine. The thebaine series (e.g. buprenorphine) is more closely related to morphine, and some members are a great deal more potent than morphine itself. The benzomorphan series (e.g. pentazocine) has rather different properties (vide infra). These heterocyclic opioid agents, of a diverse structure, act by binding to one or more of the opioid receptor sites which are to be found on neural (and some other sites) in the central and peripheral nervous systems. The opioid receptors are the natural binding sites for recognition of the endogenous members of the peptide opioid neurotransmitters families which are found in neural tissue. There are three families, which are the products of different genes: the enkephalins (principally from preproenkephalin); endorphins (from preproopiomelanocortin; POMC); and dynorphins (from preprodynorphin; preproenkephalin B). Recently, a dynorphin-like heptapeptide sequence termed nociceptin (or orphanin-FQ) has been identified which apparently is the endogenous ligand for a novel 'orphan' receptor (ORL1). There are also at least three receptor types, \L (mu), K (kappa) and 6 (delta), again each controlled by a distinct gene. [It might be noted that it has been recommended that the nomenclature for these three receptor subtypes may change, and they are expected to become known as: 6 = OP1, K = OP2, |i = OP3].The receptors are all of the seventransmembrane G-protein-coupled receptor superfamily and have largely inhibitory effects on neuronal excitability - by means of opening potassium channels or closing calcium channels, via a G-protein component in the negativecoupling to adenylyl cyclase pathway: see POTASSIUM-CHANNEL ACTIVATORS; POTASSIUM-CHANNEL BLOCKERS. Each of these three receptor subtypes can cause analgesia, and there is no exclusive relationship between the peptide family and the receptor subtype activated. However, p-endorphin is commonly most potent at Ji- and 8-receptors, whereas dynorphin A is most potent at K-receptors. The two forms of enkephalin pentapeptides - leucine- and methionineenkephalin - are potent mostly at the 5-receptors. Some opioids, including the benzomorphans (e.g. cyclazocine and pentazocine), bind appreciably to a further site, the (sigma) o-receptors that, unlike the opioid receptors detailed, have psychotomimetic potential, and patients may experience hallucinations. The a-site is best not classed as an opioid receptor site, in as much as it is not blocked by normal opioid receptor antagonists, such as naloxone - a fact of clinical importance. On the other hand, it is now clear that the ORL1 receptors are not sensitive to naloxone, though receptor activation can sometimes cause analgesia. The LI-, S- and K-receptors have been cloned, and the first three show >50% identity. Subtypes and species-dependent variants within each of these receptors have been demonstrated, but there is >90% sequence homology. The recently cloned 'orphan' receptor (ORL1) binds a dynorphinlike heptapeptide sequence. The physiological role of this
SMALL CAPS = drug families (by mechanism or application)

novel receptor is not yet apparent. Recently, gene-deletion ('knockout') experiments in mice have shown that in animals without specific opioid receptor subtypes, the effects of opioid agonists are abolished in much the expected way (e.g. Li-knockout animals do not respond to morphine). However, pain thresholds in unstressed knockout animals are unchanged, and there is no upregulation in the parallel systems (e.g. there is little upregulation of 8- and Kreceptors in Li-receptor knockout animals). The experiments have been interpreted as showing that there is little tonic modulation mediated through opioid receptors (i.e. mediated by the enkephalin/dynorphin/endorphin systems) in normal animals that are not stressed or hyperalgesic. Relative potencies of endogenous ligands, and agents selective for each of the receptor subtypes, and valuable for experimental studies, are as follows: At Li-receptors: p-endorphin > dynorphin A > [met]enkephalin = [leu]enkephalin: selective agonists include the peptides, DAMGO (also known as DAMGOL; formerly DAGO); PLO 17; and the nonpeptide sufentanyl. At 8-receptors: p-endorphin = [met]enkephalin = [leu] enkephalin > dynorphin A >: selective agonists include the peptides, DPDPE, DSBULET; DADLE; TIPP and [oAla2]-deltorphin I or II. At K-receptors: dynorphin A p-endorphin > [leu]enkephalin > [met]enkephalin: selective agonists include the nonpeptides, U 69593; U 50488; CI977; ICI 197067. At ORL1 receptors: nociceptin > dynorphin A [leu] enkephalin = [met] enkephalin. The synthetic opioid non-selective agonists etorphine is active at relatively high concentrations. See OPIOID RECEPTOR ANTAGONISTS.
Reisine, T. et al. (1993) Molecular biology of opioid receptors. Trends Neurosci., 16, 506-510. Kieffer, B.L. (1995) Recent advances in molecular recognition and signal transduction of active peptides: receptors for opioid peptides. Cell MoI. Neurobiol., 15.615-635. Mansour, A. et al. (1995) Opioid receptors: Past, present and future. Trends Neurosci., 18, 69-70. Zaki, RA. et al. (1996) Opioid receptor types and subtypes: the delta receptor as a model. Annu. Rev. Pharmacol. Toxicol., 36, 379-401. Henderson, G. ef al. (1997) The orphan opioid receptor and its endogenous ligand - nociceptin/orphanin FQ. Trends Pharmacol. Sc/., 18, 293-300. Alexander, S.P.H. et al. (1998) Receptors and ion channel nomenclature supplement. Ninth Edition. Trends Pharmacol. ScL, Suppl., 19, 1-98.

OPIOID RECEPTOR ANTAGONISTS bind at, and block, one or more of the subtypes of receptor that recognize the endogenous peptide opioids. Clinically used antagonist ligands are mostly heterocyclic derivatives of plant alkaloids related to morphine, with high affinity but low efficacy. A number of potent antagonists acting at LI-, 8- or K-receptors are available for clinical use, and are mostly active at all three receptors. They are invaluable for reversing opioid effects in routine medicine or in abuse overdose (e.g. naloxone), or in treating drug dependence (naltrexone). Naloxone is not active at (sigma) o-receptors or at ORL1 receptors. Antagonists showing some selection for each of the receptor subtypes, and valuable for experimental studies, are as follows. At ii-receptors: the peptides CTOP, CTAP and the non-peptide p-FNA (p-funaltrexamine; irreversible). At 8-receptors: the peptide ICI 174864 and the nonpeptide naltrindole. At K-receptors: nor-BNI (nor-binaltorphinine). At the recently recognized novel 'orphan' receptor, ORL1, nociceptin (or orphanin-FQ) is not antagonized by nalorphine, naloxone or any 'classsical' opioid antagonists. Some relatively subtype-nonselective experimental (nonpeptide) antagonists include: p-CNA (pchlornaltrexamine: irreversible), naltrexone or cyprodime.
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

opipramol [BAN, INN] (opipramol hydrochloride [JAN, USAN]) is a tricyclic oral ANTIDEPRESSANT.

opipramol hydrochloride -opipramol.

oprelvekin [INN] is more fully termed 2-178-interleukin 2 (human clone pXM/IL-11), and is a recombinant version of interleukin-2, a peptide cytokine inflammatory mediator, acting as a CHEMOKiNE RECEPTOR AGONIST. It can be used clinically as an IMMUNOMODULATOR, proposed for use in the prevention and treatment of cytopenia and morbid obesity. It is a derivative of human adipogenesis inhibitory factor. Opren ^ benoxaprofen. Opthaine proxymetacaine. Opticrom ^ sodium cromoglycate. Optimax ^ tryptophan. Optimine ~azatadine Opus tamoxifen. Oramorph * morphine. orange crush * bisantrene. Orap ^pimozide. Orasone ^prednisone. Or ben in ~ cloxacillin. orciprenaline [BAN, INN] (metaproterenol sulfate [USAN]; Alupent) is a (J-ADRENOCEPTOR AGONIST and is mainly used in its racemic form, which therapeutically can be used as a BRONCHODILATOR in ANTIASTHMATIC treatment. Ordrine ^ caramiphen; phenylpropanolamine hydrochloride. Orelox cefpodoxime proxetil. Oretin Methyl ^ methyltestosterone. ORF 10131 ~ norgestimate ORF 15244 ~ thymopentin. ORF 17070 -Hiistrelin. ORF 20485 - tepoxalin ORF 22164 ^atosiban. Org 483 > ethyloestrenol. Org 8 1 7 - epimestrol. Org 2969 desogestrel. Org 3770 mirtazapine. Org 32763 ^ 3-methoxyiminoquinuclidinium chloride. Organidin ~ guaiphenesin. Org OD 14 ^ tibolone. orgotein *> superoxide dismutase. Orimeten aminoglutethimide. oripavine is a thebaine alkaloid derivative from Papaver somniferum and other Papaver spp. It is an OPIOiD RECEPTOR
AGONIST With OPIOID ANALGESIC activity.

OR K 242 vadocaine. Orlaam * levacetylmethadol. ormetein A * superoxide dismutase. ornidazole [INN, USAN] is an (imidazole group) ANTIPROTOZOAL which is also used as an ANTIBACTERIAL against anaerobic bacteria. ornipressin [INN] ([Orn8]vasopressin) is a HAEMOSTATIC AGENT used as a VASOCONSTRICTOR antihaemorrhagic agent. See also argiprestocin. ornoprostil [INNJAN] (OU 1308) is a synthetic prostaglandin, a PROSTANOID RECEPTOR AGONIST reported to have potential as a GASTRIC SECRETION INHIBITOR and ANTIULCEROGENIC. It is also a dopamine release inhibitor. orotic acid [INN] (vitamin B13; whey factor; uracil-6carboxylic acid) occurs naturally in the body and is found in milk. It is a key compound involved in the biosynthesis of nucleic acid pyrimidine bases. In the form of metal salts it has been used as an ANTIHYPERLIPIDAEMIC in treating
SMALL CAPS = drug families (by mechanism or application)

hypercholesterolaemia and liver disorders. It can be used to treat hyperuricaemia and is an antigout and URICOSURiC AGENT. Also, it shows bacteriostatic and cytostatic properties. orphanin-FQ ~ nociceptin. orphenadrine [BAN, INN] (orphenadrine citrate [USAN]; orphenadrine hydrochloride; Biorphen; Disipal; Norflex) is a phenylmethoxyethanamine derivative, a MUSCARINIC CHOLINOCEPTOR ANTAGONIST used as an ANTIPARKINSONIAN AGENT in controlling tremor and rigidity. orphenadrine citrate * orphenadrine. orphenadrine hydrochloride orphenadrine. Orthoclone OKT3 muromonab-CD3. Ortho-Cream nonoxinol 9. Ortho-Dienestrol ^ dienoestrol. Ortho-Est ~ estropipate. Ortho-Gynest ^ oestriol. Orudis -*ketoprofen osalmid [INNJAN] (L 1718 and many other names) is a benzamide and has been used as a CHOLERETIC AGENT. OSanetant [INN] (SR 142801) is a substituted piperidinylmethylacetamide, a TACHYKININ RECEPTOR ANTAGONIST selective for the NK3-receptor subtype. Osteocalcin calcitonin. ostradiol dipropionate oestradiol. OtiIonium bromide [BAN, INN] is a quaternary ammonium compound, a MUSCARiNIC CHOLINOCEPTOR ANTAGONIST which can be used as a visceral ANTISPASMODIC. Otrivine-Antistin * antazoline Otrivine * xylometazoline. OU 1308 ornoprostil. ouabain [BAN] (strophanthin-G; strophanthoside-G and many other names) is a CARDIAC GLYCOSIDE, a constituent of the wood of Acokanthera oubaio and other Acokanthera spp., and seeds of several Strophanthus spp. It is a (Na/K) ATPASE INHIBITOR With ANTIARRHYTHMIC, CARDIAC STIMULANT, VASOCONSTRICTOR, HYPERTENSIVE and natriuretic activity. Ovestin oestriol. ovine prolactin ~ prolactin. ovofIavine riboflavine. OVULATION-INDUCING AGENTS are used in women as part of fertility treatment. Depending on the cause, there are four main treatments. Gonadothrophin-releasing hormone (gonadorelin; GnRH; luteinizing hormone-releasing hormone; LH-RH; or LH-FSH-RH) is a linear decapeptide, one of the hypothalamic factors that travel in a specialized system of portal blood vessels the short distance from the brain area of the hypothalamus to the adjacent anterior pituitary. Its action on the pituitary gland is to release the gonadotrophins, which are comprised of folliclestimulating hormone (FSH) and luteinizing hormone (LH). The alternative name of GnRH used in synthetic form as a drug, is gonadorelin: it is used as an infertility treatment to treat infertility (and also for amenorrhoea and diagnostic purposes - for assessing pituitary function). As explained in more detail under LH-RH RECEPTOR AGONISTS, synthetic analogues of gonadorelin (buserelin, goserelin, leuprorelin and nafarelin) can also be used to treat infertility, when they are administered by pulsatile administration (including subcutaneous or intravenous infusion and as a nasal spray). They can also be used to induce pituitary desensitization before induction of ovulation for in vitro fertilization. When used on a chronic basis they down-regulate the release system and can be used for the reverse effects, to treat endometriosis, and for breast and prostate cancer.
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

The gonadotrophins may be used directly for infertility treatment in women, when they are injected. The pituitary gonadotrophins follicle-stimulating hormone (FSH) and luteinizing hormone (LH) cause the monthly ripening in one ovary of a follicle and stimulates ovulation. These are available in several forms, e.g. menotrophin, a mix of FSH/LH, or urofollitrophin (FSH). Chorionic gonadotrophin (human chorionic gonadotrophin; HCG) is secreted by the placenta, and is prepared from the urine of pregnant women. Its main actions are those of luteinizing hormone (LH), and can be used as an infertility treatment, when it is given by intramuscular injection. The synthetic agent clomiphene is a weak antioestrogen (an 'impeded' oestrogen; structurally related to stilboestroP It is used in infertility treatment in women whose condition is linked to the persistent presence of oestrogens and a consequent failure to ovulate. Clomiphene blocks hypothalamic oestrogen receptors, so that the negative feedback of the natural oestrogen is prevented and the pituitary responds by increased secretion of gonadotrophins, which may induce ovulation. Administration is oral. See ANTIOESTROGENS. Much the same principles and agents are used in the management of fertility problems, and in manipulation of early or late seasonal pregnancy in livestock.
Fraser, H.M. et a\. (1989) Gonadotrophin-releasing hormone analogues for gynaecological disorders and infertility: a real advance. Br. Med. ]., 298, 475-476. Hodgen, G.D. (1989) General applications of GNRH agonists in gynecology: past, present and future. Obst. Gynecol. Sury., 44, 293-296. Conn, P.M. et al. (1991) Gonadotrophin-releasing hormone and its analogues. N. Engl.J. Afed.,324,93-103. Editorial (1992) New gonadotrophins for old? Lancet, 340,1442-1443.

oxabolone Cipionate [INNJAN] (Fl 5852) is a steroid with ANDROGENIC and ANABOLIC properties. oxacillin [BAN, INN] (oxacillin sodium [USAN]; Bactocill) is a semisynthetic (penicillin) ANTIBIOTIC. It can be used clinically as an ANTIBACTERIAL to treat certain infections.

oxacillin sodium ~ oxacillin oxaflozane [INN] is a non-tricyclic oral ANTIDEPRESSANT. oxagrelate [INN, USAN] is a phthalazinecarboxylate, a

(cyclic AMP) PHOSPHODIESTERASE INHIBITOR. It has PLATELET

AGGREGATION INHIBITOR and SMOOTH MUSCLE RELAXANT

properties. oxaliplatin [INN] is an organic platinum compound similar to cisplatin. It is an alkylating ANTICANCER AGENT that has been used for colorectal and ovarian cancer.

oxaprotiline [INN] (oxaprotiline hydrochloride [USAN]) is an ethanoanthracene derivative, a hydroxylated derivative of maprotiline, a tetracyclic ANTIDEPRESSANT. It acts as an (ctrsubtype) a-ADRENOCEPTOR ANTAGONIST, and can be used as an antidepressant. The (S) -form is a noradrenaline UPTAKE INHIBITOR and the (R) -form is levoprotiline [INN] (levoxaprotiline), which lacks this action. Oxaprotiline hydrochloride [USAN] is the racemate. oxaprotiline hydrochloride oxaprotiline. oxaprozin [BAN, INN, USAN] (Wy 21743) is an oxazolepropanoic acid derivative, a CYCLOOXYGENASE INHIBITOR with NSAID ANALGESIC, ANTIINFLAMMATORY and ANTIPYRETIC activity. oxazepam [BAN, INN, JAN, USAN] (Serax) is one of the [l,4]benzodiazepines and closely related to temazepam. It is a BENZODIAZEPINE BINDING-SITE AGONIST, with most of its properties similar to diazepam. It has HYPNOTIC, ANTICONVULSANT and ANXIOLYTIC activity. It is used orally for anxiety and insomnia, and to ease alcohol withdrawal. oxazidione [INN] is an (oral) ANTICOAGULANT, a synthetic agent chemically related to the coumarin group. It can be used therapeutically to prevent the formation of clots in thromboembolytic disease. oxazolam [INNJAN] (CS 300; EMD 33400) is one of the [l,4]benzodiazepines, a BENZODIAZEPINE BINDING-SITE AGONIST, with most of its properties similar to diazepam. It has HYPNOTIC, ANTICONVULSANT and ANXIOLYTIC activity. It is used orally for anxiety. OXCarbazepine [INN] (GP 47680) is a derivative of carbamazepine and with similar properties. It has been used as an ANTICONVULSANT in ANTIEPILEPTIC therapy. oxedrine [BAN] (synephrine) is a phenylethanolamine derivative, a SYMPATHOMIMETIC With VASOCONSTRICTOR, hypertensive and DECONGESTANT properties. oxetacaine oxethazaine. oxetacillin [INN] (methoxymethyl ester: sarmoxicillin [INN]) is a semisynthetic (penicillin) ANTIBIOTIC. It can be used clinically as an ANTIBACTERIAL to treat certain infections. oxethazaine [BAN, USAN] (oxetacaine [INN]; Wy 806) is an amide series LOCALANAESTHETIC, which has been used by topical application for local pain relief. It is also available combined in an ANTACID mixture (Mucaine). oxfendazole [BAN, INN, USAN] is a carbamate ANTHELMINTIC. oxibendazole [BAN, INN, USAN] is a carbamate
ANTHELMINTIC.

oxaminozoline rilmenidine.
oxamisole [INN] (oxamisole hydrochloride [USAN]) is a substituted imidazopyridine, with IMMUNOMODULATOR and ANTIVIRAL properties. oxamisole hydrochloride oxamisole. oxamniquine [BAN, INN, USAN] (Vansil) is a tetrahydroquinoline, used as an oral ANTISCHiSTOMAL AGENT. Oxandrin oxandrolone. oxandrolone [BAN, INN, JAN, USAN] (CB 8075; NSC 67068; SC 11585; Oxandrin and many other names) is a steroid, with ANDROGENiC and ANABOLIC properties. It is used orally to promote weight gain after disease or surgery. oxantel [BAN, INN] (oxantel pamoate [USAN]) is an ANTHELMINTIC that was never marketed.

oxantel pamoate * oxantel.

oxanthrazole - piroxantrone. oxantrazole * piroxantrone. oxapium iodide [INNJAN] is a quaternary ammonium
MUSCARINIC CHOLINOCEPTOR ANTAGONIST which can be used as an ANTlSPASMODIC AGENT.

oxiconazole [BAN, INN] (oxiconazole nitrate [JAN, USAN]; Oxistat) is an imidazole ANTIFUNGAL, which can be used systemically to treat a range of fungal infections. oxiconazole nitrate oxiconazole. oxidopamine * 6-hydroxydopamine. oxidronic acid [BAN, INN, USAN] is one of the bisphosphonate series of CALCIUM METABOLISM MODIFIERS used to treat disorders of bone metabolism, reducing calcium-resorption from the bone. It has been used as a diagnostic agent for bone visualization. It is a weak inhibitor of AMV reverse transcriptase and DNA-polymerase. oxiglumide -> loxiglumide. oxilofrine [INN] is an ephedrine like indirect-acting SYMPATHOMIMETIC, formerly used as an ANTIHYPOTENSIVE. oximonam [INN, USAN] (oximonam sodium [USAN]; ester = gloximonam [INN, USAN]) is a (monobactam/p-lactam) ANTIBIOTIC which shows ANTIBACTERIAL activity. oximonam sodium -* oximonam. oxindanac [INN] (CGP 6258) is an indenecarboxylic acid, a CYCLOOXYGENASE INHIBITOR with NSAID ANALGESIC,
italic = Latin or Greek; optical isomers; emphasis

SMALL CAPS = drug families (by mechanism or application)

bold = individual agents

ANTHNFLAMMATORY and ANTIPYRETIC activity. It is used as a veterinary antiinflammatory agent. oxipurinol * oxypurinol. oxiracetam [BAN, INN] (4-hydroxypiracetam; CGP 2169OE; ISF 2522) is one of the piroxicam group, and has been used as a NOOTROPlC AGENT (cognition enhancer) and investigated for the treatment of senile dementia. Oxistat * oxiconazole. oxitriptan 5-hydroxytryptophan. oxitropium bromide [BAN, INN, JAN, USAN] (scopolamine ethobromide) is a quaternary ammonium derivative of hyoscine, and is a MUSCARiNiC CHOLiNOCEPTOR ANTAGONIST which can be used by inhalation as a BRONCHODILATOR. oxmetidine [BAN, INN] (oxmetidine hydrochloride [USAN]; oxmetidine mesylate [USAN]; SKF 92994) is an imidazolylpiperonylpyrimidone, a HISTAMINE H2-RECEPTOR ANTAGONIST, GASTRIC SECRETION INHIBITOR and ANTIULCEROGENIC AGENT. oxmetidine hydrochloride oxmetidine. oxmetidine mesylate - oxmetidine. oxoallopurinol ^ oxypurinol. oxocorticosterone aldosterone. oxohydroxyoestrin oestrone. OXOmemazine [INN] (RP 6847) is one of the phenothiazine series of HISTAMINE H1-RECEPTOR ANTAGONISTS. It has SEDATIVE/TRANQUILLIZER properties, and is used as an ANTITUSSIVE, ANTIALLERGIC and antipruritic. oxophenarsine [INN] is an organic arsenical, an ANTITRYPANOSOMAL, ANTIBACTERIAL, ANTHELMINTIC and ANTICANCERAGENT. It inhibits HIV-I protein synthesis and is a sulphydryl inhibitor. y-oxophenylbutazone kebuzone 6-oxoprostaglandin E1 (6-ketoprostaglandin E1) is a vasoactive metabolite of prostacyclin. It is a PROSTANOID RECEPTOR AGONIST and a PLATELET AGGREGATION INHIBITOR. oxoprostol [BAN, INN] (MB 33153) is a synthetic prostaglandin, a PROSTANOID RECEPTOR AGONIST with potential as a GASTRIC SECRETION INHIBITOR and ANTIULCEROGENIC. OXOtremorine is a pyrrolidinone tertiary amine derivative, a MUSCARINIC CHOLINOCEPTOR AGONIST and PARASYMPATHOMIMETIC, which gains access to the CNS and is important as a convulsive pharmacological tool in the study of Parkinsonism. It is the active metabolite of tremorine. oxpentifylline [BAN] (pentoxifylline [INN, JAN, USAN]; !rental) is a theobromine derivative, a VASODILATOR that can be used orally to treat peripheral vascular disease. OXpheneridine [INN] is one of the phenylpiperidine series and is a fentanyl analogue. It is a (ji) OPIOID RECEPTOR AGONIST with OPIOID ANALGESIC and ANTISPASMODIC activity. oxprenolol [BAN, INN] (oxprenolol hydrochloride [JAN, USAN]; Trasicor) is a (subtype-non-selective) P-ADRENOCEPTOR ANTAGONIST, which is relatively lipophilic. Therapeutically, it can be used as an ANTIHYPERTENSIVE, ANTIANGINA, ANTIARRHYTHMIC and ANXIOLYTIC AGENT. oxprenolol hydrochloride oxprenolol. OX somatotropin * bovine pituitary growth hormone. Oxsoralen methoxsalen. oxybenzone [INN, USAN] (MOB; NSC 7778) is a benzophenone which is used along with other constituents in a number of topical SUNSCREEN preparations. oxybuprocaine [BAN, INN] (benoxinate hydrochloride [USAN]; Minims Benoxinate) is an ester series LOCAL ANAESTHETIC used by topical application mainly for ophthalmic use (including with fluorescein in Fluress). oxybutynin [BAN, INN] (oxybutynin hydrochloride [USAN];
SMALL CAPS = drug families (by mechanism or application)

Cystrin; Ditropan; Urotrol) is a tertiary amine MUSCARINIC CHOLINOCEPTOR ANTAGONIST, which can be used as an oral ANTlSPASMODIC, especially to treat urinary frequency, incontinence and bladder spasms. oxycinchophen [BPC, INN] (Astra 1410) is an analogue of cinchophen and is a URICOSURIC and ANTIDIURETiC AGENT. oxyclozanide [BAN, INN] is a veterinary ANTHELMINTIC. oxycodone [BAN, INN, USAN] (NSC 19043; Roxicodone) is one of the phenanthrene series, and is an OPIOiD RECEPTOR AGONIST active as an OPIOID ANALGESIC. It is used orally or by injection to treat moderately severe pain. oxyfedrine [BAN, INN] (oxyfedrine hydrochloride [JAN]) is a methoxypropiophenone derivative, a coronary VASODILATOR which can be used for ischaemic heart disease. oxyfedrine hydrochloride oxyfedrine. oxymetazoline [BAN, INN] (oxymetazoline hydrochloride [JAN, USAN]; Afrazine; Dristan) is an imidazoline derivative with (Ct1 -subtype) a-ADRENOCEPTOR AGONIST activity. It is a VASOCONSTRICTOR that can be used as a topical nasal DECONGESTANT. oxymetazoline hydrochloride ^ oxymetazoline. oxymetebanol drotebanol. oxymetholone [BAN, INN, USAN] (NSC 26198) is a steroid with ANDROGENIC and ANABOLIC properties. It is used orally to treat anaemias, including aplastic anaemias. oxymorphone [BAN, INN] (Numorphan) is one of the phenanthrene series, an OPIOID RECEPTOR AGONIST active as an OPIOID ANALGESIC. It is used by injection to treat moderate to severe pain, particularly in preoperative medication. oxypertine [BAN, INN, JAN, USAN] (Win 18501; Oxypertine) is an indole derivative with general properties similar to chlorpromazine. It is an ANTiPSYCHOTiC AGENT, used orally to treat and tranquillize patients with psychotic disorders, such as schizophrenia. The drug may also be used in the short-term treatment of severe anxiety. Oxypertine oxypertine. oxyphenbutazone [BAN, INN] (Tanderil and many other names) is one of the pyrazolone series, and a CYCLOOXYGENASE INHIBITOR with NSAID ANALGESIC, ANTIINFLAMMATORY and ANTIPYRETIC activity. As an antiinflammatory its use is restricted due to risk of severe haematological adverse effects. oxyphencyclimine [BAN, INN] (oxyphencyclimine hydrochloride [USAN]) is a tertiary amine MUSCARINiC CHOLINOCEPTOR ANTAGONIST used as a visceral ANTISPASMODIC and as an adjunct in the treatment of ulcers. oxyphencyclimine hydrochloride oxyphencyclimine. oxyphenisatin [BAN, INN] (oxyphenisatin acetate [USAN]) is a (stimulant) LAXATIVE, chemically a bishydroxyphenylindolinone related to phenolphthalein. oxyphenisatin acetate * oxyphenisatin. oxyphenonium bromide [BAN, INN] is a quaternary ammonium MUSCARINIC CHOLINOCEPTOR ANTAGONIST. It can be used as a visceral ANTiSPASMODiC, as an adjunct in the treatment of ulcers. oxypurinol [BAN, USAN] (oxipurinol [INN]; alloxanthine; oxoallopurinol; BW 55-5; NSC 76239) is a XANTHINE-OXIDASE INHIBITOR, formerly used as an antigout agent. oxytetracycline [BAN, NSI, INNJMAF] (Terramycin) is a semisynthetic (tetracycline) ANTIBIOTIC. It can be used clinically as a broad-spectrum semisynthetic oral ANTIBACTERIAL to treat certain infections. OXYTOCIC AGENTS hasten childbirth, generally by contracting the uterus. Many therapeutically useful agents do
italic = Latin or Greek; optical isomers; emphasis

bold = individual agents

so by acting as VASOPRESSiN RECEPTOR AGONISTS at the oxytocin (OT) subtype of receptors. Many analogues have been developed that are more active, or more selective than oxytocin itself, but few of these have entered therapeutics. One that has been used is demoxytocin. Some of these agents are discussed under another heading: see vasopressin receptor agonist. Oxytocin is used in its natural, but synthetic, form (Syntocinon) for the induction of labour, when it is given by intravenous infusion, or sublingually. The other main class of agent used for contractile actions on the uterus are the prostanoids. They may be used together with oxytocin for the induction of labour. Some are also used for therapeutic abortion: e.g. gcmcprost. See PROSTANOID
RECEPTOR AGONISTS.

Many other agents have actions on the uterus, including MUSCARINIC CHOLINOCEPTOR AGONISTS, 5-hydroxytryptamine (5-HT2) agonists (see 5-HYDROXYTRYPTAMINE RECEPTOR AGONISTS); a-ADRENOCEPTOR AGONISTS (which can contract the uterus); BRADYKININ RECEPTORAGONISTS (B2-receptors). However, these actions are not selective and so are not harnessed therapeutically.
Jenkins, J.S. et al. (1991) The role of oxytocin: present concepts. Clin. Endocrinol. (Oxf/. 34. 515-525. Mohr, E. et al. (1992) The hypothalamic hormone oxytocin: from gene expression to signal transduction. Rev. Physiol. Biochem. PharmacoL, 121, 31-48. Wray, S. (1993) Uterine contraction and physiological mechanisms of modulation. AmJ. Physiol., 264, C1-C18. Bossmar, T. et al. (1995) Receptor-mediated uterine effects of vasopressin and oxytocin in nonpregnant women. Br. J. Obstet. Gynaecol., 102, 907-912.

oxytocin [BAN, INN, USAN] (ct-hypophamine; Syntocinon; Vasotocin) is a cyclic nonapeptide hormone that can be obtained from posterior lobe of mammalian posterior pituitary (neurohypophysis), though the material used therapeutically is now synthetic. It is the principal uteruscontracting and milk-ejecting hormone, and can be used as an OXYTOCIC AGENT. It is agonist at oxytocin receptors ((OT) VASOPRESSIN RECEPTOR AGONIST). Clinically, it is used parenterally in the induction and augmentation of labour. The following analogues, which have been proved to be more active and more selective than oxytocin, have separate entries: desaminooxytocin; hydroxyoxytocin; nacartocin, [A3-Pro7]oxytocin; [THr4GIy7]oxytocin; [Thz7]oxytocin; [Hse4]oxytocin; treoxytocin. Arg8-oxytocin ^ argiprestocin. deamino-oxytocin * demoxytocin. [homoserine4]oxytocin [Hse4]oxytocin. [Hse4]oxytocin ([homoserine4]oxytocin) is a synthetic analogue of oxytocin and an agonist at oxytocin receptors (i.e. an (OT) VASOPRESSIN RECEPTORAGONIST), that has oxytocic activity and is more potent than oxytocin. See also argiprestocin. [IIe8]oxytocin * mesotocin. [A3-Pro7]oxytocin didehydroproline oxytocin. [Ser4,lle8]oxytocin isotocin [Thr4]oxytocin * treoxytocin. [Thr4Gly7]oxytocin is a synthetic analogue of oxytocin and agonist at oxytocin receptors (i.e. an (OT) VASOPRESSIN RECEPTOR AGONIST) that has OXYTOCIC activity and is more potent than oxytocin. [Thz7]oxytocin is a synthetic analogue of oxytocin and an agonist at oxytocin receptors (i.e. an (OT) VASOPRESSIN RECEPTOR AGONIST) that has OXYTOCIC activity and is more potent than oxytocin. [valine8]oxytocin * valitocin ozagrel [INN] is an imidazolyl derivative, a THROMBOXANE SYNTHETASE INHIBITOR, used in ANTIASTHMATIC treatment and
as an ANTITHROMBOTIC. SMALL CAPS = drug families (by mechanism or application)

P2S * pralidoxime. P83 6029A ^ velnacrine. P 638 ~ puromycin. P 652 ^ fomocaine. P 1133 -nialamide P 1888 sulphan blue. P 4125 sulphan blue. P 5048 * dimethisterone. pABA ^ aminobenzoic acid. PABA ^ aminobenzoic acid. paclitaxel [BAN, INN, USAN] (BMS 181339-01; NSC 125973; Taxol) is a taxane ANTiCANCER AGENT originally isolated from the stem bark of certain species of yew tree ( Taxus brevifolia and Taxus cuspidata (Taxaceae)), but now manufactured semisynthetically. The taxoids have a unique mode of action, and interfere with mitotic cell division. This depends on the actions of microtubules, protein polymers in continuous formation and disassembly. The taxoids promote further assembly of the polymers and inhibit depolymerization, and this disturbs mitosis in both susceptible normal and malignant cells. Paclitaxel is used by intravenous infusion as an oral anticancer treatment of ovarian and sometimes breast cancer (usually in combination with cisplatin) It has also been shown to be active against oomycete fungi. As a biochemical tool, it is extensively used to study cellular shape and function. pacrinolol [INN] is a P-ADRENOCEPTORANTAGONIST; never marketed. padimate O [USAN] is a benzoic acid ester, used extensively in SUNSCREEN preparations. Padutin kallidinogenase. pafenolol [INN] is a P-ADRENOCEPTOR ANTAGONIST. PAHA ^ aminohippuric acid. PALA * sparfosic acid. Pa If Sum ~ dextromoramide. palmidrol [INN] is a lipid compound isolated from soyabean lecithin, egg yolk and peanut meal. It has IMMUNOMODULATOR and ANTIINFLAMMATORY properties. palonosetron [INN] (palonosetron hydrochloride [USAN]; RS 42358) is a benzisoquinolinone derivative, a selective
(5-HT3) 5-HYDROXYTRYPTAMINE RECEPTOR ANTAGONIST, with

ANTIEMETIC and ANXIOLYTIC activity. palonosetron hydrochloride palonosetron. Paludrine * proguanil. PAM * pralidoxime. 2-PAM * pralidoxime. 2-PAMCI pralidoxime L-PAM * melphalan. pamaquine [INN] is an 8-aminoquinolone ANTIMALARIAL, which is no longer in extensive use. pamatolol [INN] (pamatolol sulfate [USAN]) is a

P-ADRENOCEPTOR ANTAGONIST.
pamatolol sulfate pamatolol.

Pamelor nortriptyline.
bold = individual agents italic = Latin or Greek; optical isomers; emphasis