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All about Nexium Drug Online
Pharmacological action
Inhibitor of H +-K +-ATPase. The active ingredient Nexium - esomeprazole, S-isomer of omeprazole, decreases the secretion of hydrochloric acid in the stomach by specific inhibition of acid pump in the parietal cells. S-and R-isomer of omeprazole have similar pharmacodynamic activity.
Esomeprazole is a weak base and is activated in the acidic environment of the secretory tubules parietal cells of gastric mucosa, which inhibits the activity of H +-K +-ATPase and thus blocks the final stage of secretion of hydrochloric acid. Nexium inhibits both basal and stimulated gastric secretion.
The action of the drug develops within 1 h after oral administration at a dose of 20 mg or 40 mg. When receiving the drug daily for 5 days at 20 mg 1 time / day average maximum concentration of acid in gastric contents after pentagastrin stimulation is decreased by 90% (when measuring the acid concentration in 6-7 hours after taking the dose on day 5 of therapy).
In patients with symptoms of gastroesophageal reflux disease after 5 days of daily administration Nexium orally at a dose of 20 mg or 40 mg of pH in the stomach for daily monitoring was above 4 for an average of 13 and 17 h, respectively. Among patients taking 20 mg of the drug in the day, the maintenance at the acidity level of pH above 4 for 8, 12 and 16 h was achieved in 76%, 54% and 24%, respectively. For 40 mg esomeprazole, the ratio was 97%, 92% and 56%, respectively.
Analysis of pharmacokinetic data revealed a relationship between acid secretion and the concentration of drug in plasma (the concentration used to assess the parameter AUC).
When you receive 40 mg of the drug in day cure reflux esophagitis occurs in 78% of patients after 4 weeks of therapy and in 93% - after 8 weeks of therapy.
Treatment Nexiumom a dose of 20 mg 2 times / day in combination with appropriate antibiotics for one week leads to the successful eradication of Helicobacter pylori in approximately 90% of patients.
Patients with uncomplicated duodenal ulcer after a week's course of eradication therapy does not require further treatment antisecretory therapy for healing ulcers.
The drug in plasma gastrin level is increased as a result of decreased intragastric acid secretion.
Patients who used antisecretory drugs for a long time, often observed the formation of glandular cysts in the stomach. This phenomenon is due to physiological changes as a result of inhibition of acid secretion. Cysts are benign and tend to disappear.
Due to the fact that esomeprazole is unstable in acidic medium, tablets contain granules of the active substance coated with a stable to the action of gastric juice shell.
Indications
Gastroesophageal reflux disease:
- Treatment of erosive reflux esophagitis;
- Long-term maintenance therapy to prevent relapse in patients with healed esophagitis;
- Symptomatic treatment of gastroesophageal reflux disease.
Eradication Helicobacter pylori (in combination with antibiotic therapy), as well as:
- Treatment of duodenal ulcer associated with Helicobacter pylori;
- Prevention of recurrence of peptic ulcers associated with Helicobacter pylori.
Dosage regimen
For the treatment of erosive reflux esophagitis medication prescribed in a single dose of 40 mg 1 time / day for 4 weeks. Additional 4-week course of therapy is recommended for patients when, after the first course of the disease symptoms persist.
For long-term maintenance treatment of patients with healed esophagitis to prevent relapse of drug prescribe 20 mg 1 time per day.
For the symptomatic treatment of gastroesophageal reflux disease without esophagitis medication prescribed in a dose of 20 mg 1 time per day. If after 4 weeks of treatment the symptoms do not disappear, should undertake further examination of the patient. After removing the symptoms can go to the drug treatment "if necessary", ie take Nexium 20 mg of 1 times / day in the event of symptoms prior to their withdrawal.
For the eradication of Helicobacter pylori, for the treatment of duodenal ulcer associated with Helicobacter pylori, to prevent relapse of peptic ulcers associated with Helicobacter pylori, Nexium prescribe a single dose of 20 mg, amoxicillin - 1 g, clarithromycin - 500 mg. All medications taken 2 times daily for 7 days.
In appointing the drug to patients with impaired renal function dosage adjustment is required. Be wary of the drug in patients with severe renal insufficiency due to limited clinical experience of its use in this category of patients.
In appointing Nexium patients with impaired hepatic function or mild to moderately dosage adjustment is required. Patients with severe hepatic impairment applied dose should not exceed 20 mg / day.
Elderly correction dosing regime is not required.
Tablets should be swallowed whole, washed down with liquid. Pills can not chew or crush. Patients with difficulty swallowing a pill may be dissolved in half a glass of carbonated water, stir up the splitting of tablets and drink a suspension of microgranules immediately or within 30 minutes. Then again, should fill the glass halfway with water, stir and drink residues. You should not use other liquids, as a protective shell microgranules can be dissolved. Do not chew or crush microgranules.
Side effects
In the application of esomeprazole can be expected to rare side effects of the racemic drug (omeprazole). In the conduct of clinical trials esomeprazole such effects have not been described.
In the conduct of clinical studies revealed the following side effects:
From the digestive system: frequent (> 0.01 but <0.1) - abdominal pain, diarrhea, nausea, vomiting, constipation, rarely (> 0.001 but <0.01) - a dry mouth.
From CNS: frequent (> 0.01 but <0.1) - headache, rare (> 0.001 but <0.01) - dizziness.
Dermatological reactions: rare (> 0.001 but <0.01) - dermatitis, pruritus, urticaria.
None of these effects are not dose-dependent manner.
The following adverse effects were observed in the application of the racemic drug (omeprazole) and can be expected also in the application of esomeprazole.
From the central nervous system and peripheral nervous system: paresthesia, somnolence, insomnia, dizziness, reversible mental confusion, anxiety, agitation, depression, hallucinations (mainly in severely ill patients).
From the Endocrine: gynecomastia.
From the digestive system: stomatitis, gastrointestinal candidiasis, increased activity of liver enzymes, encephalopathy in patients with prolonged severe liver disease, hepatitis with (or without), jaundice, liver failure.
The part of the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis and pancytopenia.
The part of the musculoskeletal system: joint pain, muscle weakness and myalgia.
Dermatological reactions: cyp, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, alopecia.
Allergic reaction: angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.
Other: general weakness, sweating, peripheral edema, blurred vision, changes in taste and hyponatremia.
Contraindications
- Hypersensitivity to esomeprazole, substituted benzimidazole or other components of the drug.
Pregnancy and lactation
There is currently no data on the use Nexium pregnancy. Appointment of the drug in this period is possible only if the anticipated benefits to the mother outweighs the potential risk to the fetus.
At the present time is unknown, it stands esomeprazole with breast milk, so should not be given Nexium during breastfeeding.
In animal studies did not reveal any negative effects esomeprazole for the development of an embryo or fetus. Introduction of the racemic drug also did not exert any negative impact on the animals during pregnancy, childbirth and the period of postnatal development.
Cautions
Before the appointment of esomeprazole should exclude the possibility of malignancy, since the treatment Nexiumom can lead to smoothing of symptoms and delay diagnosis.
Patients taking the drug over a long period (especially more than a year), should be under regular medical supervision.
Patients who are on the regime "treatment on demand", should be instructed to contact their physician when changing the nature of symptoms. Taking into account the fluctuations in the plasma concentration of esomeprazole in the appointment of the drug in the mode of "treatment on demand", should take into account the interaction of the drug with other drugs.
In appointing Nexium for Helicobacter pylori eradication should be taken into account the possibility of drug interactions for all components of triple therapy. Clarithromycin - a potent inhibitor of CYP3A4, therefore, must consider all contraindications and interactions clarithromycin in the case of patients taking other drugs, is metabolized with the participation of CYP3A4 (eg, cisapride).
Patients with hereditary fructose intolerance, glucose malabsorption or galaktoznoy Sucrase-izomaltaznoy insufficiency should not take this drug.
Use in Pediatrics
We do not recommend the use of drugs in children due to lack of data.
Effects on ability to drive vehicles and management mechanisms
There is no evidence the influence of the drug on the ability to drive vehicles and management mechanisms.
Overdose
There is currently no described cases of overdose. Single dose of 80 mg esomeprazole did not cause any adverse effects.
Treatment: If necessary to symptomatic and supportive therapy. The specific antidote is known. Dialysis is ineffective, because esomeprazole bound to plasma proteins.
Drug Interactions
Effect of esomeprazole on the pharmacokinetics of other drugs
In applying Nexium simultaneously with other drugs, the mechanism of absorption which depends on the acidity of the medium may decrease or increase absorption of other medicines. As well as using other drugs that suppress acid secretion or antacid, treatment of esomeprazole may reduce the absorption of ketoconazole or itraconazole.
The joint application Nexium with drugs, the metabolism of which involved CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, can lead to increased concentrations of these drugs in plasma and demand a reduction of their doses.
In joint admission Nexium and 30 mg of diazepam by 45% decreased clearance of the enzyme-cubstratnogo complex (CYP2C19-diazepam).
In an application Nexium 40 mg 13% increased the residual concentration of phenytoin in the blood plasma of patients with epilepsy (recommended to control the concentration of phenytoin in the blood plasma in the appointment of esomeprazole and its abolition).
In healthy volunteers joint reception with cisapride 40 mg Nexium led to an increase in cisapride AUC and a 32% increase in T1 / 2 cisapride at 31%, but the concentration of cisapride in plasma did not significantly change. Slight lengthening of the interval QT, which occurred in the application of monotherapy with cisapride, while adding Nexium not increased.
In an application Nexium not cause clinically significant changes in pharmacokinetic parameters of amoxicillin, quinidine, and warfarin.
Effect of drugs on the pharmacokinetics of esomeprazole.
In an application Nexium clarithromycin (500 mg 2 times / day) AUC esomeprazole increased by 2 times (Nexium dose adjustment is not required).
Conditions and terms of storage
Drug should be stored in places inaccessible to children, at a temperature below 30 ° C. Do not apply after the expiration date stated on the packaging.
Conditions of supply of pharmacies
The drug is released with a prescription.
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Inhibitor of H +-K +-ATPase. The active ingredient Nexium - esomeprazole, S-isomer of omeprazole, decreases the secretion of hydrochloric acid in the stomach by specific inhibition of acid pump in the parietal cells. S-and R-isomer of omeprazole have similar pharmacodynamic activity.
Esomeprazole is a weak base and is activated in the acidic environment of the secretory tubules parietal cells of gastric mucosa, which inhibits the activity of H +-K +-ATPase and thus blocks the final stage of secretion of hydrochloric acid. Nexium inhibits both basal and stimulated gastric secretion.
The action of the drug develops within 1 h after oral administration at a dose of 20 mg or 40 mg. When receiving the drug daily for 5 days at 20 mg 1 time / day average maximum concentration of acid in gastric contents after pentagastrin stimulation is decreased by 90% (when measuring the acid concentration in 6-7 hours after taking the dose on day 5 of therapy).
In patients with symptoms of gastroesophageal reflux disease after 5 days of daily administration Nexium orally at a dose of 20 mg or 40 mg of pH in the stomach for daily monitoring was above 4 for an average of 13 and 17 h, respectively. Among patients taking 20 mg of the drug in the day, the maintenance at the acidity level of pH above 4 for 8, 12 and 16 h was achieved in 76%, 54% and 24%, respectively. For 40 mg esomeprazole, the ratio was 97%, 92% and 56%, respectively.
Analysis of pharmacokinetic data revealed a relationship between acid secretion and the concentration of drug in plasma (the concentration used to assess the parameter AUC).
When you receive 40 mg of the drug in day cure reflux esophagitis occurs in 78% of patients after 4 weeks of therapy and in 93% - after 8 weeks of therapy.
Treatment Nexiumom a dose of 20 mg 2 times / day in combination with appropriate antibiotics for one week leads to the successful eradication of Helicobacter pylori in approximately 90% of patients.
Patients with uncomplicated duodenal ulcer after a week's course of eradication therapy does not require further treatment antisecretory therapy for healing ulcers.
The drug in plasma gastrin level is increased as a result of decreased intragastric acid secretion.
Patients who used antisecretory drugs for a long time, often observed the formation of glandular cysts in the stomach. This phenomenon is due to physiological changes as a result of inhibition of acid secretion. Cysts are benign and tend to disappear.
Due to the fact that esomeprazole is unstable in acidic medium, tablets contain granules of the active substance coated with a stable to the action of gastric juice shell.
Indications
Gastroesophageal reflux disease:
- Treatment of erosive reflux esophagitis;
- Long-term maintenance therapy to prevent relapse in patients with healed esophagitis;
- Symptomatic treatment of gastroesophageal reflux disease.
Eradication Helicobacter pylori (in combination with antibiotic therapy), as well as:
- Treatment of duodenal ulcer associated with Helicobacter pylori;
- Prevention of recurrence of peptic ulcers associated with Helicobacter pylori.
Dosage regimen
For the treatment of erosive reflux esophagitis medication prescribed in a single dose of 40 mg 1 time / day for 4 weeks. Additional 4-week course of therapy is recommended for patients when, after the first course of the disease symptoms persist.
For long-term maintenance treatment of patients with healed esophagitis to prevent relapse of drug prescribe 20 mg 1 time per day.
For the symptomatic treatment of gastroesophageal reflux disease without esophagitis medication prescribed in a dose of 20 mg 1 time per day. If after 4 weeks of treatment the symptoms do not disappear, should undertake further examination of the patient. After removing the symptoms can go to the drug treatment "if necessary", ie take Nexium 20 mg of 1 times / day in the event of symptoms prior to their withdrawal.
For the eradication of Helicobacter pylori, for the treatment of duodenal ulcer associated with Helicobacter pylori, to prevent relapse of peptic ulcers associated with Helicobacter pylori, Nexium prescribe a single dose of 20 mg, amoxicillin - 1 g, clarithromycin - 500 mg. All medications taken 2 times daily for 7 days.
In appointing the drug to patients with impaired renal function dosage adjustment is required. Be wary of the drug in patients with severe renal insufficiency due to limited clinical experience of its use in this category of patients.
In appointing Nexium patients with impaired hepatic function or mild to moderately dosage adjustment is required. Patients with severe hepatic impairment applied dose should not exceed 20 mg / day.
Elderly correction dosing regime is not required.
Tablets should be swallowed whole, washed down with liquid. Pills can not chew or crush. Patients with difficulty swallowing a pill may be dissolved in half a glass of carbonated water, stir up the splitting of tablets and drink a suspension of microgranules immediately or within 30 minutes. Then again, should fill the glass halfway with water, stir and drink residues. You should not use other liquids, as a protective shell microgranules can be dissolved. Do not chew or crush microgranules.
Side effects
In the application of esomeprazole can be expected to rare side effects of the racemic drug (omeprazole). In the conduct of clinical trials esomeprazole such effects have not been described.
In the conduct of clinical studies revealed the following side effects:
From the digestive system: frequent (> 0.01 but <0.1) - abdominal pain, diarrhea, nausea, vomiting, constipation, rarely (> 0.001 but <0.01) - a dry mouth.
From CNS: frequent (> 0.01 but <0.1) - headache, rare (> 0.001 but <0.01) - dizziness.
Dermatological reactions: rare (> 0.001 but <0.01) - dermatitis, pruritus, urticaria.
None of these effects are not dose-dependent manner.
The following adverse effects were observed in the application of the racemic drug (omeprazole) and can be expected also in the application of esomeprazole.
From the central nervous system and peripheral nervous system: paresthesia, somnolence, insomnia, dizziness, reversible mental confusion, anxiety, agitation, depression, hallucinations (mainly in severely ill patients).
From the Endocrine: gynecomastia.
From the digestive system: stomatitis, gastrointestinal candidiasis, increased activity of liver enzymes, encephalopathy in patients with prolonged severe liver disease, hepatitis with (or without), jaundice, liver failure.
The part of the hemopoietic system: leukopenia, thrombocytopenia, agranulocytosis and pancytopenia.
The part of the musculoskeletal system: joint pain, muscle weakness and myalgia.
Dermatological reactions: cyp, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, alopecia.
Allergic reaction: angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.
Other: general weakness, sweating, peripheral edema, blurred vision, changes in taste and hyponatremia.
Contraindications
- Hypersensitivity to esomeprazole, substituted benzimidazole or other components of the drug.
Pregnancy and lactation
There is currently no data on the use Nexium pregnancy. Appointment of the drug in this period is possible only if the anticipated benefits to the mother outweighs the potential risk to the fetus.
At the present time is unknown, it stands esomeprazole with breast milk, so should not be given Nexium during breastfeeding.
In animal studies did not reveal any negative effects esomeprazole for the development of an embryo or fetus. Introduction of the racemic drug also did not exert any negative impact on the animals during pregnancy, childbirth and the period of postnatal development.
Cautions
Before the appointment of esomeprazole should exclude the possibility of malignancy, since the treatment Nexiumom can lead to smoothing of symptoms and delay diagnosis.
Patients taking the drug over a long period (especially more than a year), should be under regular medical supervision.
Patients who are on the regime "treatment on demand", should be instructed to contact their physician when changing the nature of symptoms. Taking into account the fluctuations in the plasma concentration of esomeprazole in the appointment of the drug in the mode of "treatment on demand", should take into account the interaction of the drug with other drugs.
In appointing Nexium for Helicobacter pylori eradication should be taken into account the possibility of drug interactions for all components of triple therapy. Clarithromycin - a potent inhibitor of CYP3A4, therefore, must consider all contraindications and interactions clarithromycin in the case of patients taking other drugs, is metabolized with the participation of CYP3A4 (eg, cisapride).
Patients with hereditary fructose intolerance, glucose malabsorption or galaktoznoy Sucrase-izomaltaznoy insufficiency should not take this drug.
Use in Pediatrics
We do not recommend the use of drugs in children due to lack of data.
Effects on ability to drive vehicles and management mechanisms
There is no evidence the influence of the drug on the ability to drive vehicles and management mechanisms.
Overdose
There is currently no described cases of overdose. Single dose of 80 mg esomeprazole did not cause any adverse effects.
Treatment: If necessary to symptomatic and supportive therapy. The specific antidote is known. Dialysis is ineffective, because esomeprazole bound to plasma proteins.
Drug Interactions
Effect of esomeprazole on the pharmacokinetics of other drugs
In applying Nexium simultaneously with other drugs, the mechanism of absorption which depends on the acidity of the medium may decrease or increase absorption of other medicines. As well as using other drugs that suppress acid secretion or antacid, treatment of esomeprazole may reduce the absorption of ketoconazole or itraconazole.
The joint application Nexium with drugs, the metabolism of which involved CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, can lead to increased concentrations of these drugs in plasma and demand a reduction of their doses.
In joint admission Nexium and 30 mg of diazepam by 45% decreased clearance of the enzyme-cubstratnogo complex (CYP2C19-diazepam).
In an application Nexium 40 mg 13% increased the residual concentration of phenytoin in the blood plasma of patients with epilepsy (recommended to control the concentration of phenytoin in the blood plasma in the appointment of esomeprazole and its abolition).
In healthy volunteers joint reception with cisapride 40 mg Nexium led to an increase in cisapride AUC and a 32% increase in T1 / 2 cisapride at 31%, but the concentration of cisapride in plasma did not significantly change. Slight lengthening of the interval QT, which occurred in the application of monotherapy with cisapride, while adding Nexium not increased.
In an application Nexium not cause clinically significant changes in pharmacokinetic parameters of amoxicillin, quinidine, and warfarin.
Effect of drugs on the pharmacokinetics of esomeprazole.
In an application Nexium clarithromycin (500 mg 2 times / day) AUC esomeprazole increased by 2 times (Nexium dose adjustment is not required).
Conditions and terms of storage
Drug should be stored in places inaccessible to children, at a temperature below 30 ° C. Do not apply after the expiration date stated on the packaging.
Conditions of supply of pharmacies
The drug is released with a prescription.
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Wednesday, December 23, 2009
Poor planning: what to do with the rooms of irregular shape?
Rooms of irregular shape, broken ratio, failed niche ... Sometimes lay flat presents us with many surprises. But its shortcomings can be fixed independently, without resorting to radical changes.
Narrow and long
This is too elongated room is that it lacks a cozy corner and there are difficulties with the harmonious arrangement of furniture. How to solve this problem?
If the room has at least two windows along the wall, then we can divide the space into two parts, leaving each of the window. The partition between the two is often better not to do continuous or mobile (eg mobile) to maintain a sense of space. The role of partitioning can perform screen, cabinet or rack with flower plant pots. If the room only one window, then the dark part of you can make the working area with artificial lighting.
Another method of visual correction of space - the podium. It is best to place it in the remote end of the room. A short podium will provide not only a separate zone (it can be done working, equip lounge or sleeper), but also visually shorten the room. The remainder of the room you can place furniture in the usual manner.
There is another great way to make the placement of the desired shape - furniture made to order. Especially good with this task handle sliding door wardrobes, and they cleverly disguised as a wall. Furniture individual project - an excellent option for non-standard facilities (eg, attic).
Small and intimate
Visually, add the volume of small-sized rooms in several ways.
First, you can get rid of the massive door, replacing it with a mobile door-accordion. This will help neutralize the sense of closeness and isolation. Secondly, the correct approach to the selection of furniture. Magic wand for a small and cramped room will be multi-functional furniture "Transformers": retractable bed, sofa with built-in wardrobe, folding table, a bed, a loft with a working area at the bottom, etc. Thirdly, you have to play a hand mirror and transparent surfaces.
How to make the kitchen a cozy
A typical weakness of Khrushchev - a small, but often also disproportionately elongated kitchen. On this and prepare inconvenient and uncomfortable to eat. But a kitchen can be made more comfortable. Just as in the case of a close room, kitchen transformation should start with a change of conventional doors on sliding. Placement of furniture can be varied. For example, a kitchen in one line with high shelves and a table by the window.
Straight lines create the illusion of an elongated cooking a large space. Or give preference to a corner kitchen with folding table.
Interesting design move - folding bar, which can replace the table. And remember: that the room looked cozy and spacious, the interior should be decorated in bright colors.
Read more:
yrakellow
sollini
lazzira
emaros
vahhog
qarolla
weralish
garchioss
tigrenwa
bizkalit
hapliza
jivilirge
bastohutta
durenok
roguruez
Narrow and long
This is too elongated room is that it lacks a cozy corner and there are difficulties with the harmonious arrangement of furniture. How to solve this problem?
If the room has at least two windows along the wall, then we can divide the space into two parts, leaving each of the window. The partition between the two is often better not to do continuous or mobile (eg mobile) to maintain a sense of space. The role of partitioning can perform screen, cabinet or rack with flower plant pots. If the room only one window, then the dark part of you can make the working area with artificial lighting.
Another method of visual correction of space - the podium. It is best to place it in the remote end of the room. A short podium will provide not only a separate zone (it can be done working, equip lounge or sleeper), but also visually shorten the room. The remainder of the room you can place furniture in the usual manner.
There is another great way to make the placement of the desired shape - furniture made to order. Especially good with this task handle sliding door wardrobes, and they cleverly disguised as a wall. Furniture individual project - an excellent option for non-standard facilities (eg, attic).
Small and intimate
Visually, add the volume of small-sized rooms in several ways.
First, you can get rid of the massive door, replacing it with a mobile door-accordion. This will help neutralize the sense of closeness and isolation. Secondly, the correct approach to the selection of furniture. Magic wand for a small and cramped room will be multi-functional furniture "Transformers": retractable bed, sofa with built-in wardrobe, folding table, a bed, a loft with a working area at the bottom, etc. Thirdly, you have to play a hand mirror and transparent surfaces.
How to make the kitchen a cozy
A typical weakness of Khrushchev - a small, but often also disproportionately elongated kitchen. On this and prepare inconvenient and uncomfortable to eat. But a kitchen can be made more comfortable. Just as in the case of a close room, kitchen transformation should start with a change of conventional doors on sliding. Placement of furniture can be varied. For example, a kitchen in one line with high shelves and a table by the window.
Straight lines create the illusion of an elongated cooking a large space. Or give preference to a corner kitchen with folding table.
Interesting design move - folding bar, which can replace the table. And remember: that the room looked cozy and spacious, the interior should be decorated in bright colors.
Read more:
yrakellow
sollini
lazzira
emaros
vahhog
qarolla
weralish
garchioss
tigrenwa
bizkalit
hapliza
jivilirge
bastohutta
durenok
roguruez
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