NASAL DECONGESTANT

A decongestant or nasal decongestant is a type of drug which is used to relieve nasal congestion.
A common side effect of a cold or allergies is nasal congestion. When the nasal passages become swollen and
stopped up with mucus, a "stuffy" feeling results. One of the quickest ways to clear stopped-up nasal passages is
with a nasal decongestant. Some are formulated for allergies, while others are for colds.
Function
A nasal decongestant is a formula of chemicals that shrinks the blood vessels in the nasal passages. As
the vessels narrow, it prevents excess fluid from seeping into the passages and stops the lining from
swelling. As the nasal passage lining shrinks, air is free to flow in and out of the passages clearly.
Types
Nasal decongestants come in a number of forms. They are available as a topical solution that can be
inserted directly into the nose, usually through a special spray bottle or in dropper form. Decongestants
also are available in an oral tablet (pill) form. In general, the topical sprays take effect more quickly than
do the oral decongestants, but the benefits also subside more quickly.
Comparison
Both topical sprays and oral decongestants are available in over-the-counter and prescription forms. For
a common cold, the over-the-counter treatments are usually strong enough, but in more severe cases of
flu or sinus infections, a more potent treatment may be necessary. Many allergy sufferers rely on
prescription decongestants to relieve the stopped-up sensation, thinking that an over-the-counter
treatment may not be enough. A study released found in the Archives of Otolaryngology--Head & Neck
Surgery, however, revealed that in the case of one allergy type--hay fever--there was virtually no
difference between a drugstore decongestant and an expensive prescription decongestant in treating the
symptoms.
Warning
Topical nasal sprays can be addictive if used beyond the recommended time, usually three days. Also,
over time the positive effects will subside and more solution will be needed to achieve the same effect.
Eventually, the nasal congestion will become increasingly worse rather than better with continued use of
the decongestant. This condition, known as "nasal rebound," occurs when the decongestant actually
causes the blood vessels in the nasal cavity to swell. Discontinued use will decrease the swelling of the
nasal passages over time.
Side Effects
Decongestants can result in problems such as drowsiness during the day and sleep problems at night.
The drugs in the decongestant can lead to brain over stimulation, which causes a nervous feeling and
headaches. Decongestants also can raise blood pressure. Those with high blood pressure or heart
conditions should check with their doctor before using any type of nasal decongestant.

Expectorants and Mucolytic Agents

A mucolytic agent or expectorant is any agent which dissolves thick mucus and is usually used to help relieve
respiratory difficulties. It does so by hydrolyzing glycosaminoglycans, tending to break down/lower the
viscosity of mucin-containing body secretions/components. The viscosity of mucous secretions in the lungs is
dependent upon the concentrations of mucoprotein.

An expectorant (from the Latin expectorare, to expel from the chest) helps bring up mucus and other material
from the lungs, bronchi, and trachea. An example of an expectorant is guaifenesin which promotes drainage of
mucus from the lungs by thinning the mucus and lubricating the irritated respiratory tract. Sometimes the term
"expectorant" is incorrectly extended to any cough medicine.
Antitussives
A cough medicine (or linctus, when in syrup form) is a medicinal drug used in an attempt to treat coughing and related
conditions. For dry coughs, treatment with cough suppressants (antitussives) may be attempted to suppress the body's
urge to cough, while in productive coughs (coughs that produce phlegm), treatment is attempted with expectorants
(typically guaifenesin, in most commercial medications) in an attempt to loosen mucus from the respiratory tract.

Tuberculosis Medications
Tuberculosis treatment usually requires the use of several different antibiotics that must be taken for at least six
months. Occasionally, the medications used for tuberculosis may cause side effects such as orange urine, sensitivity
to the sun, and reduced effectiveness of birth control pills and implants.
In most people, medication will cure tuberculosis if the correct drugs are taken for the right amount of time.
Tuberculosis treatment usually combines several different antibiotic medications that are given for at least 6 months,
and sometimes for as long as 12 months. This is because there are many tuberculosis bacteria (Mycobacterium
tuberculosis) that need to be killed.

FIRST-LINE MEDICATIONS
Ethambutol (commonly abbreviated EMB or simply E) is a bacteriostatic antimycobacterial drug
prescribed to treat tuberculosis. It is usually given in combination with other tuberculosis drugs, such as
isoniazid, rifampicin and pyrazinamide.
It is sold under the trade names Myambutol and Servambutol.

Mechanism of action

Ethambutol is bacteriostatic against actively growing TB bacilli. It works by obstructing the formation of cell
wall. Mycolic acids attach to the 5'-hydroxyl groups of D-arabinose residues of arabinogalactan and form
mycolyl-arabinogalactan-peptidoglycan complex in the cell wall. It disrupts arabinogalactan synthesis by
inhibiting the enzyme arabinosyl transferase. Disruption of the arabinogalactan synthesis inhibits the formation
of this complex and leads to increased permeability of the cell wall.

Adverse effects

 Optic neuritis. Hence contraindicated in children below 6 yrs of age.

 Red-green color blindness
 Peripheral neuropathy
 Arthralgia
 Hyperuricaemia
 vertical nystagmus
 milk skin reaction

Isoniazid (Laniazid, Nydrazid), also known as isonicotinylhydrazine (INH), is an organic compound

that is the first-line antituberculosis medication in prevention and treatment. It was first discovered in 1912, and
later in 1951 it was found to be effective against tuberculosis. Isoniazid is never used on its own to treat active
tuberculosis because resistance quickly develops. Isoniazid also has an antidepressant effect, and it was one of
the first antidepressants discovered.
The compound was first synthesised in the early 20th century,but its activity against tuberculosis was first
reported in the early 1950s and three pharmaceutical companies attempted unsuccessfully to simultaneously
patent the drug(the most prominent one being Roche, who launched their version, Rimifon, in 1952). With the
introduction of isoniazid, a cure for tuberculosis was first considered reasonable.

Isoniazid is available in tablet, syrup, and injectable forms (given intramuscularly or intravenously). Isoniazid is
available worldwide, is inexpensive and is generally well tolerated. It is manufactured from isonicotinic acid,

Mechanism of action

Isoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is
called KatG. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This
complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural
enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid,
required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of Isoniazid,
including nitric oxide,which has also been shown to be important in the action of another antimycobacterial
prodrug PA-824.

Isoniazid is bactericidal to rapidly-dividing mycobacteria but is bacteriostatic if the mycobacterium is slow-

growing. Isoniazid inhibits the P450 system.

Side effects

Adverse reactions include rash, abnormal liver function tests, hepatitis, sideroblastic anemia, high anion gap
metabolic acidosis, peripheral neuropathy, mild central nervous system (CNS) effects, drug interactions
resulting in increased phenytoin (Dilantin) or disulfiram (Antabuse) levels and intractable seizures (status
epilepticus).

Pyrazinamide
is a drug used to treat tuberculosis. The drug is largely bacteriostatic, but can be bacteriocidal on
actively replicating tuberculosis bacteria.

Medical uses
Pyrazinamide is only used in combination with other drugs such as isoniazid and rifampicin in the treatment of
Mycobacterium tuberculosis. It is never used on its own. It has no other indicated medical uses. In particular, it
is not used to treat other mycobacteria; Mycobacterium bovis and Mycobacterium leprae are innately resistant
to pyrazinamide. Pyrazinamide is used in the first two months of treatment to reduce the duration of treatment
required. Regimens not containing pyrazinamide must be taken for nine months or more.
Pyrazinamide in conjunction with rifampin is a preferred treatment for latent tuberculosis.
Pyrazinamide is a potent antiuricosuric drug and consequently has an off-label use in the diagnosis of causes of
hyperuricemia and hyperuricosuria. It acts on URAT1.
Mechanism of action
Pyrazinamide is a prodrug that stops the growth of Mycobacterium tuberculosis.
M. tuberculosis has the enzyme pyrazinamidase which is only active in acidic conditions. Pyrazinamidase
converts pyrazinamide to the active form, pyrazinoic acid which accumulates in the bacilli. Pyrazinoic acid was
thought to inhibit the enzyme fatty acid synthase (FAS) I, which is required by the bacterium to synthesise fatty
acids although this has been discounted. It was also suggested that the accumulation of pyrazinoic acid disrupts
membrane potential and interferes with energy production, necessary for survival of M. tuberculosis at an acidic
site of infection. Further studies reproduced the results of FAS I inhibition as the putative mechanism first in
whole cell assay of replicating M. tuberculosis bacilli which have shown that pyrazinoic acid and its ester
inhibit the synthesis of fatty acids. This study was followed by in vitro assay of tuberculous FAS I enzyme that
tested the activity with pyrazinamide, pyrazinoic acid and several classes of pyrazinamide analogs.
Pyrazinamide and its analogs inhibited the activity of purified FAS I. Mutations of the pyrazinamidase gene
(pncA) are responsible for pyrazinamide resistance in M. tuberculosis.

Side effects
The most common (approximately 1%) side effect of pyrazinamide is joint pains (arthralgia), but this is not
usually so severe that patients need to stop taking the pyrazinamide. The arthralgia can be distressing to
patients, but is never harmful.
The most dangerous side effect of pyrazinamide is hepatotoxicity, which is dose related. The old dose for
pyrazinamide was 40–70 mg/kg daily and the incidence of drug-induced hepatitis has fallen significantly since
the recommended dose has been reduced. In the standard four-drug regimen (isoniazid, rifampicin,
pyrazinamide, ethambutol), pyrazinamide is the most common cause of drug-induced hepatitis. It is not possible
to clinically distinguish pyrazinamide-induced hepatitis from hepatitis caused by isoniazid or rifampicin; test
dosing is required (this is discussed in detail in tuberculosis treatment)
Other side effects include nausea and vomiting, anorexia, sideroblastic anemia, skin rash, urticaria, pruritus,
hyperuricemia, dysuria, interstitial nephritis, malaise; rarely porphyria, and fever.

Rifampicin (INN) or rifampin (USAN) is a bactericidal antibiotic drug of the rifamycin group. It is a
semisynthetic compound derived from Amycolatopsis rifamycinica (formerly known as Amycolatopsis
mediterranei and Streptomyces mediterranei). Rifampicin may be abbreviated R, RMP, RA, RF, or RIF (US).

Pharmacodynamics (mechanism of action)

Rifampicin inhibits DNA-dependent RNA polymerase in bacterial cells by binding its beta-subunit, thus
preventing transcription to RNA and subsequent translation to proteins.[10] Its lipophilic nature makes it a good
candidate to treat the meningitis form of tuberculosis, which requires distribution to the central nervous system
and penetration through the blood-brain barrier.

Adverse effects

The most serious adverse effect is related to rifampicin's hepatotoxicity, and patients receiving
rifampicin often undergo baseline and frequent liver function tests to detect liver damage.
The more common unwanted effects include fever, gastrointestinal disturbances, rashes, and
immunological reactions.
Taking rifampicin can cause certain bodily fluids, such as urine and tears, to become orange-red in
color, a benign side effect which can be frightening if it is not expected and prepared for. This effect may also
be used to monitor effective absorption of the drug (if drug color is not seen in the urine, the patient may wish
to move the drug dose farther in time from food or milk intake). The discolorizion of sweat and tears is not
directly noticeable, but sweat may stain light clothing orange, and tears may permanently stain soft contact
lenses.
Since rifampicin may be excreted in breast milk, breast feeding should be avoided while it is being taken.

Adverse effects include:

 Hepatotoxic - Hepatitis, jaundice, liver failure in severe cases

 Respiratory - breathlessness
 Cutaneous - flushing, pruritus, rash, redness and watering of eyes
 Abdominal - nausea, vomiting, abdominal cramps with or without diarrhea
  Flu-like symptoms - with chills, fever, headache, arthralgia, and malaise. Rifampin has good penetration
into the brain, and this may directly explain some malaise and dysphoria in a minority of users.

Rifapentine
Rifapentine is an antibiotic drug that treats pulmonary tuberculosis (TB). Treatment begins in an
intensive phase of twice-weekly dosing, followed by a maintenance phase of once-weekly dosing.
The drug's brand name is Prifkin, and it is marketed by Sanofi-Aventis. It was approved by the Food and
Drug Administration in June 1998.

Uses/Indications
Rifapentine is used in combination with other medications for the treatment of tuberculosis. It is not
recommended for patients who are HIV positive; those with cavitary lesions; or patients with extra-pulmonary
involvement. Those patients are considered high risk and due to the increased treatment failure and relapse rates
associated with rifapentine-based vs rifampin-based treatment, rifapentine use is not recommended.
Side Effects
These side effects require immediate attention from a physician:
 Loss of appetite
 Fever
 Dark color of urine
 Feeling of general discomfort
 Nausea or vomiting
 Yellow skin or eyes
 Pain or swelling in the joints
If severe or constant diarrhea develops, the patient should contact a physician immediately.
Because rifapentine is taken with other medications, the following list of side effects may be shared with any of
the other drugs used for the treatment of tuberculosis:
 Blood in urine
 Itchiness
 Loss of iron in the body
 Loss of appetite
 Skin breakouts
 Rash
 Nausea and vomiting
 Pain, including joint pain
Rifapentine can change the color of some body fluids such as the saliva, urine, breast milk, tears, and sweat to
an orange-red. The skin, teeth, and tongue may also change color. Dentures and contact lenses can be
permanently stained.

Rifabutin
Rifabutin is an antibiotic. It prevents bacteria from multiplying in your body.
Rifabutin is used to prevent mycobacterium avium complex (MAC) in people with HIV (human
immunodeficiency virus) infection. Rifabutin is also used with other medications to treat tuberculosis in people
with HIV.
Rifabutin is often given together with other antibiotics.

Rifabutin Side Effects

Call your doctor at once if you have any of these serious side effects:
 severe skin rash or itching
 pale skin, weakness, easy bruising or bleeding
  fever, chills, body aches, flu symptoms; or
 eye pain or redness, vision loss
Less serious side effects may include:
 red, orange, or brown discoloration of your skin, tears, sweat, saliva, urine, or stools
 nausea, vomiting, diarrhea
 stomach pain
 belching, bloating, loss of appetite
 headache; or
 mild skin rash or itching

SECOND-LINE MEDICATIONS
Amikacin
is an aminoglycoside antibiotic used to treat different types of bacterial infections. Amikacin works by
binding to the bacterial 30S ribosomal subunit, causing misreading of mRNA and leaving the bacterium unable
to synthesize proteins vital to its growth.
Administration
Amikacin may be administered once or twice a day but must be given by the intravenous or intramuscular route.
There is no oral form available as amikacin is not absorbed orally. In people with kidney failure, dosage must
be adjusted according to the creatinine clearance, usually by reducing the dosing frequency.
Uses
Amikacin is most often used for treating severe, hospital-acquired infections with multidrug resistant Gram
negative bacteria such as Pseudomonas aeruginosa, Acinetobacter, and Enterobacter.
Amikacin may be combined with a beta-lactam antibiotic for empiric therapy for people with neutropenia and
fever.
Resistance
Amikacin has high resistance against bacterial inactivation. It resists attacks by most bacterial inactivating
enzymes, this is accomplished by the L-hydroxyaminobuteroyl amide (L-HABA) moiety attached to N-3 which
inhibits acetylation, phosphorylation and adenylation in the distant amino sugar ring (C-2,C-3,C-4). To prevent
the development of bacterial resistance to this extremely powerful antibiotic, its use is tightly regulated.
Side effects
Side effects of amikacin are similar to other aminoglycosides. Kidney damage and hearing loss are the most
important effects. Because of this potential, blood levels of the drug and markers of kidney function (creatinine)
may be monitored. Moreover, doses are adjusted specifically based upon serum Creatinine clearance in clinical
settings

Capreomycin
is an antibiotic that fights bacteria in the body.
Capreomycin is used to treat Mycobacterium tuberculosis.
Capreomycin is usually given after other tuberculosis medications have been tried without successful treatment
of the infection.
Capreomycin may also be used for other purposes not listed in this medication guide.

capreomycin is a peptide antibiotic, commonly grouped with the aminoglycosides, which is given in
combination with other antibiotics for tuberculosis. Adverse effects include nephrotoxicity and 8th cranial nerve
toxicity. The drug should not be given with streptomycin or other drugs that may damage the 8th nerve.
Side effects of Capreomycin

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing;
swelling of your face, lips, tongue, or throat.

Stop using capreomycin and call your doctor at once if you have any of these serious side effects:

 urinating less than usual or not at all

 changes in your hearing
 spinning sensation, problems with balance
 ringing or roaring sound in your ears; or
 low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle
weakness or limp feeling)

Less serious side effects may include:

 mild skin rash

 fever, chills, body aches, flu symptoms; or
 pain, swelling, or a hard lump where the injection was given