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Description

Phenylpropanolamine has been withdrawn in Canada and the United States. In November 2000, the Food and Drug
Administration (FDA) issued a public health advisory against the use of the drug.

Pharmacology
Indication

For the treatment of nasal congestion, control of urinary incontinence, priapism and obesity.

Pharmacodynamics Phenylpropanolamine (PPA), a sympathomimetic agent structurally similar to pseudoephedrine, is used to treat
nasal congestion. Phenylpropanolamine is found in appetite suppressant formulations and with guaifenesinin in
cough-cold formulations. In 2000, the FDA requested that all drug companies discontinue marketing products
containing phenylpropanolamine, due to an increased risk of hemorrhagic stroke in women who used
phenylpropanolamine.
Mechanism of
action

Phenylpropanolamine acts directly on alpha- and, to a lesser degree, beta-adrenergic receptors in the mucosa of the
respiratory tract. Stimulation of alpha-adrenergic receptors produces vasoconstriction, reduces tissue hyperemia,
edema, and nasal congestion, and increases nasal airway patency. PPA indirectly stimulates beta-receptors,
producing tachycardia and a positive inotropic effect.

Absorption

Reduced bioavailability (about 38%) from gastrointestinal tract because of first pass metabolism by monoamine
oxidase in the stomach and liver.

asthma and hay fever. Once the mast cell-antibody-antigen complex is formed. hay fever. it generally causes less drowsiness and sedation than promethazine. rhinitis. DB09440) Type Small Molecule Groups Approved Description A histamine H1 antagonist used in allergic reactions. histamine can react with local or widespread tissues through histamine receptors. Histamine. [PubChem] Pharmacology Indication For the treatment of rhinitis. allergy. Once released. urticaria. Pharmacodynamics In allergic reactions an allergen interacts with and cross-links surface IgE antibodies on mast cells and basophils. One of the most widely used of the classical antihistaminics. common cold. It has also been used in veterinary applications. and asthma. a complex series of events occurs that eventually leads to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil.NAME CHLORPHENAMINE Accession Number DB01114 (APRD00001. urticaria. acting on H 1- .

and runny nose due to hay fever and other upper respiratory allergies. produces pruritis. and bronchoconstriction. hypotension. which subsequently leads to temporary relief of the negative symptoms brought on by histamine. is a histamine H1 antagonis (or more correctly. headache.receptors. an inverse histamine agonist) of the alkylamine class. vasodilatation. Chlorpheniramine. NAME METHYLPREDNISOLONE Accession Number DB00959 (APRD00342) Type Small Molecule Groups Approved . Absorption Well absorbed in the gastrointestinal tract. This blocks the action of endogenous histamine. Histamine also increases vascular permeability and potentiates pain. It provides effective. temporary relief of sneezing. watery and itchy eyes. Mechanism of action Chlorpheniramine binds to the histamine H1 receptor. tachycardia. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract. blood vessels and respiratory tract. flushing.

which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Mechanism of action Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins. are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents. interfere with mediators of inflammatory response. By this mechanism. Absorption Oral bioavailability 80-99% Name Acetaminophen . modifying transcription and protein synthesis.Description A prednisolone derivative with similar anti-inflammatory action Pharmacology Indication Adjunctive therapy for short-term administration in rheumatoid arthritis. lipocortins. glucocorticoids can inhibit leukocyte infiltration at the site of inflammation. Pharmacodynamics Methylprednisolone and its derivatives. methylprednisolone sodium succinate and methylprednisolone acetate.

At therapeutic doses acetaminophen does not irritate the lining of the stomach nor affect blood coagulation. Acetaminophen. but because of its wide availability. minor aches. unlike other common analgesics such as aspirin and ibuprofen. also known as paracetamol. Acetaminophen and NSAIDs . headaches. has no anti-inflammatory properties or effects on platelet function. deliberate or accidental overdoses are not uncommon. It is extremely safe in standard doses. Like NSAIDs and unlike opioid analgesics. or the fetal ductus arteriosus (as NSAIDs can). It is a major ingredient in numerous cold and flu medications and many prescription analgesics. and pains. Its therapeutic effects are similar to salicylates. Pharmacodynamics Acetaminophen (USAN) or Paracetamol (INN) is a widely used analgesic and antipyretic drug that is used for the relief of fever. and it is not a member of the class of drugs known as non-steroidal anti-inflammatory drugs or NSAIDs. but it lacks anti-inflammatory. is commonly used for its analgesic and antipyretic effects. kidney function. acetaminophen does not cause euphoria or alter mood in any way. antiplatelet. and other minor aches and pains. and gastric ulcerative effects Indication For temporary relief of fever.Accession Number DB00316 (APRD00252) Type Small Molecule Groups Approved Description Acetaminophen.

Absorption Rapid and almost complete . but future research may provide further insight into how it works. thus. has no peripheral anti-inflammatory affects. Acetaminophen is used on its own or in combination with pseudoephedrine. sweating and hence heat dissipation. studies have found that acetaminophen indirectly blocks COX. Its exact mechanism of action is still poorly understood. increasing the pain threshold by inhibiting both isoforms of cyclooxygenase. or oxycodone. and that this blockade is ineffective in the presence of peroxides. and COX-3 enzymes involved in prostaglandin (PG) synthesis. hydrocodone. This enzyme is now referred to as COX-3. tolerance and withdrawal. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site. diphenhydramine. acetaminophen does not inhibit cyclooxygenase in peripheral tissues and. chlorpheniramine. dextromethorphan. The antipyretic properties of acetaminophen are likely due to direct effects on the heat-regulating centres of the hypothalamus resulting in peripheral vasodilation. COX-2. Mechanism of action Acetaminophen is thought to act primarily in the CNS. codeine. doxylamine. dependence. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides.have the benefit of being completely free of problems with addiction. COX-1. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. Unlike NSAIDs.